imidazolidines

Summary

Summary: Compounds based on reduced IMIDAZOLINES which contain no double bonds in the ring.

Top Publications

  1. ncbi Interaction of azimilide with neurohumoral and channel receptors
    R R Brooks
    Procter and Gamble Pharmaceuticals, 11810 E Miami River Rd, Cincinnati, OH 45252, USA
    Biochem Pharmacol 62:883-92. 2001
  2. ncbi Deletion of aldose reductase leads to protection against cerebral ischemic injury
    Amy C Y Lo
    Department of Anatomy, The University of Hong Kong, Hong Kong SAR, China
    J Cereb Blood Flow Metab 27:1496-509. 2007
  3. pmc Aldose reductase inhibition counteracts oxidative-nitrosative stress and poly(ADP-ribose) polymerase activation in tissue sites for diabetes complications
    Irina G Obrosova
    Pennington Biomedical Research Center, Louisiana State University, 6400 Perkins Rd, Baton Rouge, LA 70808, USA
    Diabetes 54:234-42. 2005
  4. pmc Inhibition of aldose reductase prevents colon cancer metastasis
    Ravinder Tammali
    Department of Biochemistry and Molecular Biology, University of Texas Medical Branch, Galveston, TX 77555, USA
    Carcinogenesis 32:1259-67. 2011
  5. ncbi Gene deletion and pharmacological inhibition of aldose reductase protect against retinal ischemic injury
    Alvin K H Cheung
    Department of Anatomy, The University of Hong Kong, Pokfulam Road, Hong Kong, China
    Exp Eye Res 85:608-16. 2007
  6. ncbi Studies of rat and human retinas predict a role for the polyol pathway in human diabetic retinopathy
    Zeina Dagher
    Harvard Medical School, Schepens Eye Research Institute, 20 Staniford St, Boston, MA 02114, USA
    Diabetes 53:2404-11. 2004
  7. pmc Anti-inflammatory effect of aldose reductase inhibition in murine polymicrobial sepsis
    Aramati B M Reddy
    Department of Biochemistry and Molecular Biology, University of Texas Medical Branch, Galveston, TX 77555, USA
    Cytokine 48:170-6. 2009
  8. ncbi Role of aldose reductase and oxidative damage in diabetes and the consequent potential for therapeutic options
    Satish K Srivastava
    Department of Human Biological Chemistry and Genetics, University of Texas Medical Branch, Galveston, Texas 77555, USA
    Endocr Rev 26:380-92. 2005
  9. pmc Amelioration of acute kidney injury in lipopolysaccharide-induced systemic inflammatory response syndrome by an aldose reductase inhibitor, fidarestat
    Kazunori Takahashi
    Department of Pathology and Molecular Medicine, Hirosaki University Graduate School of Medicine, Hirosaki, Japan
    PLoS ONE 7:e30134. 2012
  10. pmc Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, CHUQ, Hôpital Saint François d Assise, Québec, Québec, Canada
    J Med Chem 54:4559-80. 2011

Research Grants

  1. Role of poly(ADP-ribosyl)ation in diabetic neuropathy
    IRINA OBROSOVA; Fiscal Year: 2003
  2. Na+/H+-exchanger-1 and Diabetic Neuropathy
    IRINA OBROSOVA; Fiscal Year: 2009
  3. Peroxynitrite decomposition catalyst:diabetic neuropathy
    IRINA OBROSOVA; Fiscal Year: 2006
  4. Poly(ADP-ribose) polymerase in diabetic nephropathy
    IRINA OBROSOVA; Fiscal Year: 2006
  5. 12/15-Lipoxygenase and Diabetic Neuropathy
    IRINA OBROSOVA; Fiscal Year: 2009
  6. 12/15-Lipoxygenase and Diabetic Neuropathy
    IRINA OBROSOVA; Fiscal Year: 2009
  7. Peroxynitrite, protein nitration and advanced diabetic neuropathy
    Irina G Obrosova; Fiscal Year: 2010
  8. Na+/H+-exchanger-1 and Diabetic Neuropathy
    Irina G Obrosova; Fiscal Year: 2010
  9. 12/15-Lipoxygenase and Diabetic Neuropathy
    Irina G Obrosova; Fiscal Year: 2010
  10. MEASUREMENT ERRORS IN CANCER EPIDEMIOLOGY
    Bernard Rosner; Fiscal Year: 2002

Detail Information

Publications155 found, 100 shown here

  1. ncbi Interaction of azimilide with neurohumoral and channel receptors
    R R Brooks
    Procter and Gamble Pharmaceuticals, 11810 E Miami River Rd, Cincinnati, OH 45252, USA
    Biochem Pharmacol 62:883-92. 2001
    ..14 microM for carbachol). Azimilide's receptor interactions occur at concentrations from one to forty times those required to block cardiac delayed-rectifier channels but could contribute to the efficacy and safety of the drug...
  2. ncbi Deletion of aldose reductase leads to protection against cerebral ischemic injury
    Amy C Y Lo
    Department of Anatomy, The University of Hong Kong, Hong Kong SAR, China
    J Cereb Blood Flow Metab 27:1496-509. 2007
    ....
  3. pmc Aldose reductase inhibition counteracts oxidative-nitrosative stress and poly(ADP-ribose) polymerase activation in tissue sites for diabetes complications
    Irina G Obrosova
    Pennington Biomedical Research Center, Louisiana State University, 6400 Perkins Rd, Baton Rouge, LA 70808, USA
    Diabetes 54:234-42. 2005
    ..These findings reveal the new beneficial properties of fidarestat, thus further justifying the ongoing clinical trials of this specific, potent, and low-toxic ARI...
  4. pmc Inhibition of aldose reductase prevents colon cancer metastasis
    Ravinder Tammali
    Department of Biochemistry and Molecular Biology, University of Texas Medical Branch, Galveston, TX 77555, USA
    Carcinogenesis 32:1259-67. 2011
    ..Thus, our results indicate that AR regulates cancer cell adhesion, invasion and migration events which initiate metastasis and therefore, AR inhibition could be a novel therapeutic approach for the prevention of colon cancer metastasis...
  5. ncbi Gene deletion and pharmacological inhibition of aldose reductase protect against retinal ischemic injury
    Alvin K H Cheung
    Department of Anatomy, The University of Hong Kong, Pokfulam Road, Hong Kong, China
    Exp Eye Res 85:608-16. 2007
    ..Therefore, AR inhibition should be considered for the treatment of retinal ischemic injury often observed in diabetic patients...
  6. ncbi Studies of rat and human retinas predict a role for the polyol pathway in human diabetic retinopathy
    Zeina Dagher
    Harvard Medical School, Schepens Eye Research Institute, 20 Staniford St, Boston, MA 02114, USA
    Diabetes 53:2404-11. 2004
    ..Excess aldose reductase activity can be a mechanism for human diabetic retinopathy...
  7. pmc Anti-inflammatory effect of aldose reductase inhibition in murine polymicrobial sepsis
    Aramati B M Reddy
    Department of Biochemistry and Molecular Biology, University of Texas Medical Branch, Galveston, TX 77555, USA
    Cytokine 48:170-6. 2009
    ..Our aim is to investigate the effect of AR inhibitors on the prevention of inflammatory cytokines in the cecum ligation and puncture (CLP) model of polymicrobial sepsis which closely mimics the sepsis syndrome in humans...
  8. ncbi Role of aldose reductase and oxidative damage in diabetes and the consequent potential for therapeutic options
    Satish K Srivastava
    Department of Human Biological Chemistry and Genetics, University of Texas Medical Branch, Galveston, Texas 77555, USA
    Endocr Rev 26:380-92. 2005
    ....
  9. pmc Amelioration of acute kidney injury in lipopolysaccharide-induced systemic inflammatory response syndrome by an aldose reductase inhibitor, fidarestat
    Kazunori Takahashi
    Department of Pathology and Molecular Medicine, Hirosaki University Graduate School of Medicine, Hirosaki, Japan
    PLoS ONE 7:e30134. 2012
    ..Aldose reductase (AR) inhibitor is recently found to suppress lipopolysaccharide (LPS)-induced cardiac failure and its lethality. We studied the effects of AR inhibitor on LPS-induced acute kidney injury and its mechanism...
  10. pmc Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4
    Sebastien Fortin
    Unité des Biotechnologies et de Bioingénierie, Centre de Recherche, CHUQ, Hôpital Saint François d Assise, Québec, Québec, Canada
    J Med Chem 54:4559-80. 2011
    ..PIB-SOs were subjected to CoMFA and CoMSIA analyses to establish quantitative structure-activity relationships...
  11. doi Biological and immunological activity of new imidazolidines against adult worms of Schistosoma mansoni
    Juliana Kelle de Andrade Lemoine Neves
    Laboratório de Planejamento e Síntese de Fármacos LPSF do Departamento de Antibióticos UFPE, Recife, Pernambuco, Brazil
    Parasitol Res 107:531-8. 2010
    ..RZS-2) and LPSF/5-(4-fluoride-benzylidene-3-(4-nitrebenzyl)-4-thioxo-imidazolidin-2-one (RZS-5) imidazolidines, against adult worms of Schistosoma mansoni...
  12. doi The role of the polyol pathway in acute kidney injury caused by hindlimb ischaemia in mice
    Soroku Yagihashi
    Department of Pathology and Molecular Medicine, Hirosaki University Graduate School of Medicine, Hirosaki, Japan
    J Pathol 220:530-41. 2010
    ..Thus, these findings suggest that the polyol pathway is implicated in AKI caused by ischaemic limb injury and that AR may be a potential therapeutic target for this condition...
  13. ncbi Suppression of choroidal neovascularization by inhibiting angiotensin-converting enzyme: minimal role of bradykinin
    Norihiro Nagai
    Laboratory of Retinal Cell Biology, Keio University School of Medicine, Tokyo, Japan
    Invest Ophthalmol Vis Sci 48:2321-6. 2007
    ..The purpose of the present study was to investigate the role of bradykinin in the development of choroidal neovascularization (CNV), with or without ACE inhibition...
  14. ncbi A potent aldose reductase inhibitor, (2S,4S)-6-fluoro-2', 5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide (Fidarestat): its absolute configuration and interactions with the aldose reductase by X-ray crystallography
    M Oka
    Rational Drug Design Laboratories, 4 1 1, Misato, Matsukawa machi, Fukushima 960 1242, Japan
    J Med Chem 43:2479-83. 2000
    ..Explanations for the differences between the observed activities of fidarestat and its stereoisomer 2 were suggested by computer modeling...
  15. ncbi Aldose reductase inhibitor fidarestat prevents retinal oxidative stress and vascular endothelial growth factor overexpression in streptozotocin-diabetic rats
    Irina G Obrosova
    Division of Endocrinology and Metabolism, Department of Internal Medicine, University of Michigan Medical Center, 1150 West Medical Center Drive, MSRB II, Room 5570, Ann Arbor, MI 48109 0678, USA
    Diabetes 52:864-71. 2003
    ..In conclusion, increased AR activity contributes to retinal oxidative stress and VEGF protein overexpression in early diabetes. The findings justify the rationale for evaluation of fidarestat on diabetic retinopathy...
  16. ncbi A role for the polyol pathway in the early neuroretinal apoptosis and glial changes induced by diabetes in the rat
    Veronica Asnaghi
    Schepens Eye Research Institute and Department of Ophthalmology, Harvard Medical School, Boston, Massachusetts 02114, USA
    Diabetes 52:506-11. 2003
    ..These findings have implications for how to evaluate the role of the polyol pathway in diabetic retinopathy...
  17. ncbi An aldose reductase inhibitor reverses early diabetes-induced changes in peripheral nerve function, metabolism, and antioxidative defense
    Irina G Obrosova
    Division of Endocrinology and Metabolism, Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor, Michigan 48109 0354, USA
    FASEB J 16:123-5. 2002
    ..In conclusion, treatment with adequate doses of ARIs (that is, doses that completely inhibit increased sorbitol pathway activity) is an effective approach for reversal of, at least, early diabetic neuropathy...
  18. ncbi Important role of nitric oxide in the effect of angiotensin-converting enzyme inhibitor imidapril on vascular injury
    Rui Chen
    Department of Medical Biochemistry, Ehime University School of Medicine, Shigenobu, Onsen gun, Ehime 791 0295, Japan
    Hypertension 42:542-7. 2003
    ..These results indicate that not only blockade of angiotensin II production but also activation of the bradykinin-NO system plays an important role in the beneficial effects of imidapril on vascular remodeling...
  19. ncbi Clinical efficacy of fidarestat, a novel aldose reductase inhibitor, for diabetic peripheral neuropathy: a 52-week multicenter placebo-controlled double-blind parallel group study
    N Hotta
    Third Department of Internal Medicine, Nagoya University School of Medicine, Nagoya, Japan
    Diabetes Care 24:1776-82. 2001
    ..The purpose of this study was to evaluate the efficacy of fidarestat, a novel aldose reductase (AR) inhibitor, in a double-blind placebo controlled study in patients with type 1 and type 2 diabetes and associated peripheral neuropathy...
  20. ncbi Long-term treatment with fidarestat suppresses the development of diabetic retinopathy in STZ-induced diabetic rats
    Noriaki Kato
    Central Research Laboratory, Sanwa Kagaku Kenkyusho Co, Ltd, 363 Shiosaki, Hokusei, Mie 511 0406, Inabe, Japan
    J Diabetes Complications 17:374-9. 2003
    ..These results suggest that fidarestat, by virtue of its long-term correction of the accelerated polyol pathway, has a potential role in preventing the progression of diabetic retinopathy...
  21. ncbi [The inhibitory effect of aldose reductase inhibitor for proliferation in the lens epithelial cells of rat sugar cataract]
    Soichi Morikubo
    Department of Ophthalmology, Fukui Medical University, 23 3 Shimoaizuki, Matsuoka machi, Yoshida gun, Fukui 910 1193, Japan
    Nihon Ganka Gakkai Zasshi 107:565-70. 2003
    ..To evaluate the inhibitory effect of aldose reductase inhibitor (ARI) for the accumulation of sugar alcohol and the enhanced proliferation of lens epithelial cells of rats fed a galactose diet...
  22. ncbi Symptoms at the time of arrhythmia recurrence in patients receiving azimilide for control of atrial fibrillation or flutter: results from randomized trials
    Stuart J Connolly
    Department of Medicine, McMaster University, Hamilton, Ontario, Canada
    Am Heart J 146:489-93. 2003
    ..This paper examines the data collected during those studies regarding the symptoms reported by patients at the time of AF recurrence..
  23. ncbi Angiotensin II and oxidative stress in Dahl Salt-sensitive rat with heart failure
    Akihiro Tojo
    Division of Nephrology and Endocrinology, Department of Internal Medicine, University of Tokyo, Tokyo, Japan
    Hypertension 40:834-9. 2002
    ..In conclusion, DSHF rats showed increased oxidative stress in the kidney via NAD(P)H oxidase. Blockade of local angiotensin II with subpressor dose of imidapril inhibited NAD(P)H oxidase and prevented renal damage...
  24. ncbi Risk of proarrhythmia with class III antiarrhythmic agents: sex-based differences and other issues
    Deborah L Wolbrette
    Department of Medicine, The Milton S Hershey Medical Center, Penn State University College of Medicine, Hershey, Pennsylvania 17033, USA
    Am J Cardiol 91:39D-44D. 2003
    ....
  25. pmc Effect of severe renal impairment on the pharmacokinetics of azimilide following single dose oral administration
    Alfred E Corey
    Procter and Gamble Pharmaceuticals, Health Care Research Center, 8700 Mason Montgomery Road, Mason, OH 45040 9462, USA
    Br J Clin Pharmacol 54:449-52. 2002
    ..To assess the influence of severe renal impairment on azimilide pharmacokinetics...
  26. ncbi Asymptomatic or "silent" atrial fibrillation: frequency in untreated patients and patients receiving azimilide
    Richard L Page
    Cardiovascular Division, Clinical Cardiac Electrophysiology, Department of Internal Medicine, The University of Texas Southwestern Medical Center, Dallas, USA
    Circulation 107:1141-5. 2003
    ....
  27. ncbi Pure class III agents for prevention of sudden cardiac death
    Craig M Pratt
    Department of Medicine, Baylor College of Medicine, Houston, Texas, USA
    J Cardiovasc Electrophysiol 14:S82-6. 2003
    ..These trials play pivotal roles for regulatory approval of these drugs for use in atrial fibrillation...
  28. ncbi The effect of isoproterenol on the class III effect of azimilide in humans
    Paul Dorian
    Department of Medicine, St Michael s Hospital, Toronto, Canada
    J Cardiovasc Pharmacol Ther 7:211-7. 2002
    ..Azimilide is an investigational class III antiarrhythmic agent that blocks both IKr and IKs...
  29. ncbi Aldose reductase mediates cytotoxic signals of hyperglycemia and TNF-alpha in human lens epithelial cells
    Kota V Ramana
    Department of Human Biological Chemistry and Genetics, University of Texas Medical Branch, Galveston, Texas 77555 0647, USA
    FASEB J 17:315-7. 2003
    ..These observations could provide new insights into the pathophysiology of diabetes and the role of aberrant glucose metabolism in apoptotic cell death...
  30. ncbi Effects of aldose reductase inhibitors and galactose withdrawal on fluorescein angiographic lesions in galactose-fed dogs
    Michael Cusick
    National Eye Institute, National Institutes of Health, and Howard Hughes Medical Institute National Institutes of Health Research Scholars Program, Bethesda, MD 20892, USA
    Arch Ophthalmol 121:1745-51. 2003
    ....
  31. ncbi Oral class III antiarrhythmics: what is new?
    Mazhar H Khan
    Department of Medicine, Pennsylvania State University, College of Medicine, The Milton S Hershey Medical Center, Hershey 17033, USA
    Curr Opin Cardiol 19:47-51. 2004
    ..This review describes the latest developments in the clinical usage of class III antiarrhythmics. It also discusses some new studies providing insight into the mechanism of action of these drugs...
  32. ncbi High-resolution structures of human aldose reductase holoenzyme in complex with stereoisomers of the potent inhibitor Fidarestat: stereospecific interaction between the enzyme and a cyclic imide type inhibitor
    Ossama El-Kabbani
    Department of Medicinal Chemistry, Victorian College of Pharmacy, Monash University Parkville Campus, 381 Royal Parade, Parkville, VIC 3052, Australia
    J Med Chem 47:4530-7. 2004
    ....
  33. ncbi Atrial-selective antiarrhythmic actions of novel Ikur vs. Ikr, Iks, and IKAch class Ic drugs and beta blockers in pigs
    Karsten Knobloch
    DG Cardiovascular Diseases, Aventis Pharma, Frankfurt am Main, Germany
    Med Sci Monit 10:BR221-8. 2004
    ....
  34. ncbi Mitogen-activated protein kinase p38 mediates reduced nerve conduction velocity in experimental diabetic neuropathy: interactions with aldose reductase
    Sally A Price
    Division of Neuroscience, School of Biological Sciences, University of Manchester, Stopford Building 1 124, Oxford Road, Manchester M13 9PT, UK
    Diabetes 53:1851-6. 2004
    ..Insulin and aldose reductase inhibitors can prevent excess polyol pathway flux, and hence these agents may prevent NCV deficits by preventing p38 MAP kinase activation...
  35. ncbi Diverse effects of long-term treatment with imidapril and irbesartan on cell growth signal, apoptosis and collagen type I expression in the left ventricle of spontaneously hypertensive rats
    Jin Ming Wang
    Department of Cardiology, Renmin Hospital, Wuhan University School of Medicine, Wuhan 430060, People s Republic of China
    Life Sci 75:407-20. 2004
    ..Irbesartan is more effective in regressing the homeostasis between ERK-1 and MKP-1, however imidapril is superior in suppressing apoptosis and collagen synthesis in cardiac tissue...
  36. ncbi Influence of azimilide on CYP2C19-mediated metabolism
    Mohamed El Mouelhi
    Procter and Gamble Pharmaceuticals, Mason, OH 45040 9462, USA
    J Clin Pharmacol 44:373-8. 2004
    ....
  37. ncbi Effect of imidapril, an angiotensin-converting enzyme inhibitor, on fructose-induced insulin resistance in rats
    Tsuneyuki Oda
    Research Center of Health, Physical Fitness and Sports, Nagoya University, Nagoya, Japan
    Endocr J 51:69-74. 2004
    ....
  38. ncbi Mortality in patients after a recent myocardial infarction: a randomized, placebo-controlled trial of azimilide using heart rate variability for risk stratification
    A John Camm
    Department of Cardiology, St George s Hospital, London, UK
    Circulation 109:990-6. 2004
    ..Azimilide, a novel class III antiarrhythmic drug, was investigated for its effects on mortality in patients with depressed LVF after recent MI and in a subpopulation of patients with low HRV...
  39. ncbi Trials of new antiarrhythmic drugs for maintenance of sinus rhythm in patients with atrial fibrillation
    Steven Singh
    Veterans Affairs Center, Washington, USA
    J Interv Card Electrophysiol 10:71-6. 2004
    ..Tedisamil is a complex class 3 agent, blocking multiple channels. Piboserod is a selective 5-HT receptor antagonist that is being investigated in clinical trials...
  40. ncbi Azimilide for atrial fibrillation: clinical trial results and implications
    Edward L C Pritchett
    Department of Medicine, Division of Clinical Pharmacology, Duke University Medical Center, Durham, North Carolina, USA
    Card Electrophysiol Rev 7:215-9. 2003
    ..Infrequent cases of torsade de pointes and severe neutropenia were reported in patients taking azimilide. Azimilide is an investigational antiarrhythmic drug that has shown efficacy in patients with atrial fibrillation...
  41. ncbi Suppression of 3-deoxyglucosone and heparin-binding epidermal growth factor-like growth factor mRNA expression by an aldose reductase inhibitor in rat vascular smooth muscle cells
    Weiguo Li
    Division of Metabolic Diseases, Nagoya University Graduate School of Medicine, Nagoya, Japan
    Biochem Biophys Res Commun 314:370-6. 2004
    ..The results suggest that the polyol pathway may play a substantial role in SMC hyperplasia under hyperglycemic condition in part by affecting HB-EGF mRNA expression via the production of carbonyl compounds and oxidative stress...
  42. ncbi [Progress in the clinical use of anti-arrhythmic drugs (I)]
    Wan zhen Li
    Zhonghua Er Ke Za Zhi 41:735-7. 2003
  43. ncbi The efficacy of azimilide in the treatment of atrial fibrillation in the presence of left ventricular systolic dysfunction: results from the Azimilide Postinfarct Survival Evaluation (ALIVE) trial
    Craig M Pratt
    The Methodist DeBakey Heart Center and Department of Medicine, Section of Cardiology, Baylor College of Medicine, Houston, Texas 77030, USA
    J Am Coll Cardiol 43:1211-6. 2004
    ....
  44. ncbi Azimilide decreases recurrent ventricular tachyarrhythmias in patients with implantable cardioverter defibrillators
    Igor Singer
    University of Louisville, Division of Cardiology, Louisville, Kentucky, USA
    J Am Coll Cardiol 43:39-43. 2004
    ..This study evaluated the effects of azimilide dihydrochloride (AZ) on anti-tachycardia pacing (ATP) and shock-terminated events in patients with implantable cardioverter defibrillators (ICDs)...
  45. ncbi Ultrahigh resolution drug design. II. Atomic resolution structures of human aldose reductase holoenzyme complexed with Fidarestat and Minalrestat: implications for the binding of cyclic imide inhibitors
    Ossama El-Kabbani
    Department of Medicinal Chemistry, Victorian College of Pharmacy, Monash University Parkville Campus, Parkville, Victoria, Australia
    Proteins 55:805-13. 2004
    ..These observations suggest a mechanism in which Fidarestat is bound protonated and becomes negatively charged by donating the proton to His110, which may have important implications on drug design...
  46. ncbi Regulation of vascular smooth muscle cell growth by aldose reductase
    A Bhatnagar
    Division of Cardiology, Department of Medicine, Jewish Cardiovascular Research Center, University of Louisville, 500 South Floyd Street, 40202, Louisville, KY, USA
    Chem Biol Interact 130:627-36. 2001
    ..Together, these observations suggest that, in vascular smooth muscle cells (VSMC), AR is a growth-responsive gene product and that inhibition of AR prevents VSMC growth and decreases intimal hyperplasia and restenosis...
  47. pmc Effect of treating streptozotocin-induced diabetic rats with sorbinil, myo-inositol or aminoguanidine on endoneurial blood flow, motor nerve conduction velocity and vascular function of epineurial arterioles of the sciatic nerve
    Lawrence J Coppey
    Veterans Affairs Medical Center, Department of Internal Medicine, University of Iowa, Iowa City 52246, USA
    Int J Exp Diabetes Res 3:21-36. 2002
    ..These studies suggest that sorbinil treatment may be more effective in preventing neural dysfunction in diabetes than either aminoguanidine or myo-inositol...
  48. ncbi Antihypertensive agents prevent nephrosclerosis and left ventricular hypertrophy induced in rats by prolonged inhibition of nitric oxide synthesis
    N Akuzawa
    Second Department of Internal Medicine, Gunma University School of Medicine, Maebashi, Japan
    Am J Hypertens 11:697-707. 1998
    ....
  49. ncbi Synthesis and aldose reductase inhibitory activity of 5-arylidene-2,4-thiazolidinediones
    G Bruno
    Dipartimento Ch Inorg, Chim Anal e Ch Fis, Facoltà Scienze MMFFNN, Universita di Messina, Salita Sperone 31, 98166, Messina, Italy
    Bioorg Med Chem 10:1077-84. 2002
    ....
  50. ncbi Effect of imidapril on myocardial remodeling in L-NAME-induced hypertensive rats is associated with gene expression of NOS and ACE mRNA
    N Kobayashi
    Department of Medicine, Dokkyo University School of Medicine, Mibu, Tochigi, Japan
    Am J Hypertens 13:199-207. 2000
    ..Myocardial remodeling in L-NAME-induced hypertensive rats was significantly ameliorated by a subdepressor dose of imidapril, which may be due to an increase in local eNOS mRNA expression and a decrease in angiotensin II in the LV...
  51. ncbi Pathogenesis of diabetic neuropathy--do hyperglycemia and aldose reductase inhibitors affect neuroactive steroid formation in the rat sciatic nerves?
    A Colciago
    Department of Endocrinology, University of Milano, Italy
    Exp Clin Endocrinol Diabetes 110:22-6. 2002
    ..We conclude that hyperglycemia or the administration of the AR inhibitors do not affect 3alpha-HSD activity in peripheral nerves and therefore do not reduce the formation of steroid metabolites possibly endowed with neurotrophic action...
  52. ncbi Dose-response relations of azimilide in the management of symptomatic, recurrent, atrial fibrillation
    S J Connolly
    Department of Medicine, McMaster University, Hamilton, Ontario, Canada
    Am J Cardiol 88:974-9. 2001
    ..9% of patients receiving either of the 2 effective doses. Thus, doses of azimilide <100 mg/day are not effective for control of AF, whereas doses of 100 and 125 mg/day are effective with an acceptable risk of serious toxicity...
  53. ncbi A population pharmacokinetic-pharmacodynamic analysis and model validation of azimilide
    L Phillips
    Cognigen Corporation, Williamsville, NY, USA
    Clin Pharmacol Ther 70:370-83. 2001
    ..The relationship between azimilide concentration and change in QTc is primarily dependent on serum potassium...
  54. pmc Identification of biochemical pathways for the metabolism of oxidized low-density lipoprotein derived aldehyde-4-hydroxy trans-2-nonenal in vascular smooth muscle cells
    S Srivastava
    Experimental Research Laboratories, Division of Cardiology, University of Louisville, and Jewish Hospital Heart and Lung Institute, Louisville, KY 40202, USA
    Atherosclerosis 158:339-50. 2001
    ..These metabolic pathways may be the key regulators of the vascular effects of HNE and oxidized LDL...
  55. ncbi Effects of azimilide, a new class III antiarrhythmic drug, on reentrant circuits causing ventricular tachycardia and fibrillation in a canine model of myocardial infarction
    H Schmitt
    Department of Pharmacology, Center of Molecular Therapeutics, College of Physicians and Surgeons of Columbia University, New York, New York 10032, USA
    J Cardiovasc Electrophysiol 12:1025-33. 2001
    ..CONCLUSION: Azimilide has antiarrhythmic effects to prevent reentry causing SVT and VF in a canine infarct model...
  56. ncbi Effects of imidapril on endothelin-1 and ACE gene expression in failing hearts of salt-sensitive hypertensive rats
    N Kobayashi
    Department of Medicine, Dokkyo University School of Medicine, Mibu, Tochigi, Japan
    Am J Hypertens 13:1088-96. 2000
    ....
  57. ncbi Efficacy of azimilide and dofetilide in the dog right atrial enlargement model of atrial flutter
    M Restivo
    Cardiology Division, State University of New York Health Sciences Center at Brooklyn and Brooklyn Veterans Administration Medical Center, USA
    J Cardiovasc Electrophysiol 12:1018-24. 2001
    ..Efficacy relied on a similar mechanism of differentially prolonged refractoriness in the slow conduction component of the reentrant circuit where drug-induced termination occurred...
  58. ncbi Acidification alters antiarrhythmic drug blockade of the ether-a-go-go-related Gene (HERG) Channels
    De Li Dong
    Department of Pharmacology, Harbin Medical University, Heilongjiang Key Laboratory of Bio pharmaceutical engineering, Harbin, 150086, P R China
    Basic Clin Pharmacol Toxicol 94:209-12. 2004
    ..5 was similar to that under pH 7.5 (n=6). Acidification markedly potentiated dofetilide blockade of the HERG channels but weakened the inhibitory effects of quinidine and azimilide...
  59. ncbi Tissue Angiotensin-converting enzyme activity plays an important role in pressure overload-induced cardiac fibrosis in rats
    Yukie Kurosawa
    Discovery Research Laboratory, Tanabe Seiyaku Co, Ltd, 2 2 50 Kawagishi, Toda shi, Saitama 335 8505, Japan
    J Cardiovasc Pharmacol 39:600-9. 2002
    ..These results suggest that the increased local ACE expression contributes to the development of pressure overload-induced cardiac fibrosis but is not responsible for hypertrophy in rats...
  60. ncbi A 'specificity' pocket inferred from the crystal structures of the complexes of aldose reductase with the pharmaceutically important inhibitors tolrestat and sorbinil
    A Urzhumtsev
    UPR de Biologie Structurale 9004 IGMBC CNRS INSERM ULP 1 rue Laurent Fries, B P 163, 67404, Illkirch, France
    Structure 5:601-12. 1997
    ..The inhibitor zopolrestat binds to this anionic site, and in the hydrophobic cleft, after a change of conformation which opens a 'specificity' pocket...
  61. ncbi New antiarrhythmic drugs for the treatment of atrial fibrillation
    Antonio Castro
    Department of Heart Disease, S Filippo Neri Hospital, Rome, Italy
    Pacing Clin Electrophysiol 25:249-59. 2002
  62. ncbi [Drug therapy of ventricular arrhythmias - a contemporary perspective]
    G C Grönefeld
    Johann Wolfgang Goethe Universitat, Medizinische Klinik IV, Frankfurt am Main, Germany
    Dtsch Med Wochenschr 127:2280-4. 2002
  63. ncbi Electrophysiological and antiarrhythmic effects of the novel I(Kur) channel blockers, S9947 and S20951, on left vs. right pig atrium in vivo in comparison with the I(Kr) blockers dofetilide, azimilide, d,l-sotalol and ibutilide
    Karsten Knobloch
    DG Cardiovascular Diseases, Aventis Parma, Industriepark Hochst, Frankfurt am Main, Germany
    Naunyn Schmiedebergs Arch Pharmacol 366:482-7. 2002
    ..In contrast to selective I(Kr) blockade, I(Kur) blockade inhibited left atrial vulnerability and had no effect on the QT-interval. Thus, blockade of I(Kur) seems to be a promising atrial selective antiarrhythmic concept...
  64. ncbi Nitric oxide prevents aldose reductase activation and sorbitol accumulation during diabetes
    Deepak Chandra
    Department of Human Biological Chemistry and Genetics, University of Texas Medical Branch, Galveston, USA
    Diabetes 51:3095-101. 2002
    ..Thus, increasing NO availability may be a useful strategy for inhibiting the polyol pathway and preventing the development of diabetes complications...
  65. ncbi Aldose reductase mediates mitogenic signaling in vascular smooth muscle cells
    Kota V Ramana
    Department of Human Biological Chemistry and Genetics, University of Texas Medical Branch, Galveston, Texas 77555, USA
    J Biol Chem 277:32063-70. 2002
    ..Collectively, these data suggest that inhibition of NF-kappa B may be a significant cause of the antimitogenic effects of AR inhibition and that this may be related to disruption of PKC-associated signaling in the AR-inhibited cells...
  66. ncbi ["Diabetic autonomic neuropathy" series. Epidemiology, pathogenesis, basic therapy and prognosis]
    D Luft
    Abt Innere Medizin IV, Med Universitäts und Poliklinik, Eberhard Karls Universitat, Tubingen
    MMW Fortschr Med 144:47-50. 2002
  67. ncbi Pharmacological properties of fidarestat, a potent aldose reductase inhibitor, clarified by using sorbitol in human and rat erythrocytes
    H Sobajima
    Department of Internal Medicine, Ogaki Municipal Hospital, Gifu, Japan
    Pharmacology 62:193-9. 2001
    ..These results suggest that fidarestat potently inhibits the increase in sorbitol pathway flux in diabetic patients independent of various factors and that erythrocyte sorbitol is useful for its estimation...
  68. ncbi Fidarestat (SNK-860), a potent aldose reductase inhibitor, normalizes the elevated sorbitol accumulation in erythrocytes of diabetic patients
    Tomoichiro Asano
    Department of Internal Medicine, Faculty of Medicine, University of Tokyo, 7 3 1 Hongo, Bunkyo ku, 113, Tokyo, Japan
    J Diabetes Complications 16:133-8. 2002
    ..Further studies are needed to clarify how much the occurrence and progression of diabetic neuropathy are inhibited by normalizing sorbitol elevation with fidarestat treatment...
  69. ncbi Oxidized aldose reductase: in vivo factor not in vitro artifact
    C E Grimshaw
    Whittier Diabetes Program, Department of Medicine, University of California at San Diego, La Jolla, 92093 0983, USA
    Arch Biochem Biophys 327:89-97. 1996
    ....
  70. ncbi Antiarrhythmic effects of azimilide in paroxysmal supraventricular tachycardia: efficacy and dose-response
    Richard L Page
    Department of Medicine, Cardiovascular Division, University of Texas Southwestern Medical Center, Parkland Memorial Hospital, Dallas, Tex 75390 9047, USA
    Am Heart J 143:643-9. 2002
    ..Its effect on paroxysmal supraventricular tachycardia (PSVT) has not been reported...
  71. ncbi Synthesis, crystal structure and anticancer activity of novel derivatives of ethyl 1-(4-oxo-8-aryl-4,6,7,8-tetrahydroimidazo[2,1-c][1,2,4]triazin-3-yl)formate
    Krzysztof Sztanke
    Department of Synthesis and Technology of Drugs, Professor Feliks Skubiszewski Medical University, Lublin, Poland
    Eur J Med Chem 41:539-47. 2006
    ..The title compounds were obtained by two independent synthesis methods from 1-aryl-2-hydrazono-imidazolidines (1-aryl-2-hydrazino-imidazolines) (1-6) by cyclocondensation reaction with diethyl 2-(hydroxyimino)malonate (A)..
  72. ncbi 1H-nuclear magnetic resonance determination of the enantiomeric purity of aliphatic primary amines, beta-aminoalcohols, beta-diamines and alpha-amino-acids with 1R-(-)-myrtenal: scope and limitations
    Francois Dufrasne
    Laboratoire de Chimie Pharmaceutique Organique, Institut de Pharmacie, Universite Libre de Bruxelles, CP 205 5, Campus Plaine, B 1050, Brussels, Belgium
    Spectrochim Acta A Mol Biomol Spectrosc 59:1239-45. 2003
    ..imines were completely formed after 12 h and analysed by 1H-NMR except for N-methyl beta-diamines for which imidazolidines were obtained...
  73. ncbi A stereoselective entry into functionalized 1,2-diamines by zinc-mediated homologation of alpha-aminoacids
    Cam Thuy Hoang
    Laboratoire de Chimie des Procedes et Substances Naturelles, Institut de Chimie Moléculaire et des Matériaux d Orsay UMR CNRS 8182, Batiment 410, Université de Paris Sud 11, F 91405 Orsay, France
    Org Lett 9:2521-4. 2007
    A general, stereoselective synthesis of 4,5-disubstituted imidazolidines-2-ones from alpha-aminoacids has been developed: the key steps are a Blaise reaction of bromoacetate on alpha-aminonitriles and further reduction...
  74. ncbi Guanabenz, guanochlor, guanoxan and idazoxan bind with high affinity to non-adrenergic sites in pig kidney membranes
    P Vigne
    Centre de Biochimie du CNRS, Nice, France
    Eur J Pharmacol 160:295-8. 1989
    ..These binding sites may be the normal target of a series of imidazolidines derivatives (guanabenz, guanochlor, guanoxan), which are known for their antihypertensive properties.
  75. ncbi Synthesis of 2,3,5,6-tetrahydro-3H-imidazo[2,1-b] [1,3,5]benzotriazepines and their oxidative ring contraction into 1-(4,5-dihydro-1H-imidazol-2-yl)-1H-benzimidazoles
    Franciszek Saczewski
    Department of Chemical Technology of Drugs, Medical University of Gdansk, 80 416 Gdansk, Poland
    Farmaco 60:127-34. 2005
    ..1,3,5]benzotriazepine derivatives 3a-g were performed by reacting 2-(2-aminoarylimino)imidazolidines 1a-b with corresponding aryl aldehydes...
  76. ncbi Dynamic kinetic asymmetric cycloadditions of isocyanates to vinylaziridines
    Barry M Trost
    Department of Chemistry, Stanford University, Stanford, California 94305 5080, USA
    J Am Chem Soc 125:11836-7. 2003
    ..The products were easily reduced almost quantitatively to the sensitive imidazolidines which can be readily hydrolyzed to the vicinal diamines...
  77. doi Diamine-free lithiation-trapping of N-Boc heterocycles using s-BuLi in THF
    Graeme Barker
    Department of Chemistry, University of York, Heslington, York YO10 5DD, UK
    Org Lett 12:4176-9. 2010
    ..Subsequent electrophilic trapping or transmetalation-Negishi coupling delivered a range of functionalized pyrrolidines, imidazolidines, and piperazines in 43-83% yield.
  78. doi Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors
    J N Cumming
    Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 18:3236-41. 2008
    ..The key feature of both series is a cyclic amine motif specifically crafted to achieve interactions with both the flap and with the S2' pocket...
  79. ncbi Insecticidal and neuroblocking potencies of variants of the imidazolidine moiety of imidacloprid-related neonicotinoids and the relationship to partition coefficient and charge density on the pharmacophore
    Shinzo Kagabu
    Department of Chemistry, Faculty of Education, Gifu University, Gifu 501 1193, Japan
    J Agric Food Chem 55:812-8. 2007
    ..The equation for the insecticidal versus neuroblocking potencies indicated that both potencies are related proportionally with each other when the other factors are the same...
  80. ncbi Effects of imidapril on left ventricular mass in chronic hemodialysis patients
    Nobuko Matsumoto
    Department of Hypertension and Cardiorenal Medicine, Dokkyo Medical University, Tochigi, Japan
    Hypertens Res 29:253-60. 2006
    ..05) but was unchanged in the placebo group (129 +/- 6 to 126 +/- 5 g/m2). These results suggest that an ACE inhibitor reduces left ventricular mass in hemodialysis patients by a mechanism that is independent of changes in blood pressure...
  81. pmc Amelioration of experimental autoimmune uveoretinitis by aldose reductase inhibition in Lewis rats
    Umesh C S Yadav
    Department of Biochemistry and Molecular Biology, University of Texas Medical Branch, Galveston, Texas 77555, USA
    Invest Ophthalmol Vis Sci 52:8033-41. 2011
    ..They have now investigated the efficacy of AR inhibitors in the prevention of experimental autoimmune-induced uveitis (EAU) in rats...
  82. ncbi Medium effects on the decarboxylation of a biotin model in pure and mixed solvents from QM/MM simulations
    Orlando Acevedo
    Department of Chemistry, Yale University, 225 Prospect Street, New Haven, Connecticut 06520 8107, USA
    J Org Chem 71:4896-902. 2006
    ....
  83. ncbi The role of polyol pathway in high glucose-induced endothelial cell damages
    Tomokazu Oyama
    Center of Diabetes, Endocrine and Metabolism, Sakura Hospital, School of Medicine, Toho University, 564 1 Shimoshizu, Sakura City, Chiba, Japan
    Diabetes Res Clin Pract 73:227-34. 2006
    ..These results suggest that high glucose-induced endothelial cell damages may be mediated by activation of the polyol pathway accompanied by augmented oxidative stress...
  84. ncbi New imidazolidinic bioisosters: potential candidates for antischistosomal drugs
    Maira G R Pitta
    Departamento de Antibioticos, Universidade Federal de Pernambuco, Av Prof Moraes Rego, 50670 901 Recife, PE, Brazil
    Mem Inst Oswaldo Cruz 101:313-6. 2006
    ..These observations suggest a strong electronic contribution of the arylazo grouping in the biological response...
  85. doi Primaquine dipeptide derivatives bearing an imidazolidin-4-one moiety at the N-terminus as potential antimalarial prodrugs
    Nuno Vale
    CIQUP, Departamento de Quimica, Faculdade de Ciencias, Universidade do Porto, R Campo Alegre, P 4169 007 Porto, Portugal
    Eur J Med Chem 44:2506-16. 2009
    ....
  86. doi Watchful waiting beats androgen deprivation therapy in early prostate cancer
    Vicki Brower
    J Natl Cancer Inst 100:1494-6. 2008
  87. ncbi Synthesis and activity of 1,3,5-triphenylimidazolidine-2,4-diones and 1,3,5-triphenyl-2-thioxoimidazolidin-4-ones: characterization of new CB1 cannabinoid receptor inverse agonists/antagonists
    Giulio G Muccioli
    Unite de Chimie pharmaceutique et de Radiopharmacie, Ecole de Pharmacie, Faculte de Medecine, Universite Catholique de Louvain, Avenue E Mounier 73, UCL CMFA 7340, B 1200 Brussels, Belgium
    J Med Chem 49:872-82. 2006
    ....
  88. ncbi Imidaprilat, an angiotensin-converting enzyme inhibitor exerts neuroprotective effect via decreasing dopamine efflux and hydroxyl radical generation induced by bisphenol A and MPP+ in rat striatum
    Toshio Obata
    Department of Analytical Chemistry, School of Pharmaceutical Sciences, Ohu University, Koriyama, Fukushima 963 8611, Japan
    Brain Res 1071:250-3. 2006
    ..These results suggest that ACE inhibitors may protect against the synergistic effect of bisphenol A and MPP(+)-induced OH formation via suppressing DA efflux in the rat striatum...
  89. doi Synthesis and antimalarial activity of 2-guanidino-4-oxoimidazoline derivatives
    Xianjun Liu
    Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States
    J Med Chem 54:4523-35. 2011
    ..The metabolic stability and metabolites profile indicated that the new deoxo-IZ derivatives (8) may act as prodrugs of the corresponding IZ (1 and 2) derivatives...
  90. ncbi Hartree-Fock, Møller-Plesset calculations and dynamic NMR study of 3,3-dimethoxy-1-(imidazolidin-2-ylidene)propan-2-one
    Ali Hassanzadeh
    Department of Chemistry, Faculty of Sciences, University of Urmia, 57159, Urmia, Iran
    Spectrochim Acta A Mol Biomol Spectrosc 68:1236-43. 2007
    ..Moreover, MP2/3-21G, 6-31G calculation has not significant influence on (13)C NMR chemical shifts with respect to RHF-6-31G...
  91. doi Aldose reductase inhibitors in the treatment of diabetic peripheral neuropathy: a review
    Kate E Schemmel
    Mercy Medical Center, Dubuque, IA 52001, USA
    J Diabetes Complications 24:354-60. 2010
    ..The purpose of this article was to examine how aldose reductase (AR) inhibitors are used in the prevention and treatment of peripheral neuropathy in diabetes, specifically focusing on efficacy...
  92. doi Imidaprilat inhibits matrix metalloproteinase-2 activity in human cardiac fibroblasts induced by interleukin-1beta via NO-dependent pathway
    Xiao gang Guo
    Department of Cardiovascular Science, The First Affiliated Hospital, College of Medicine, Zhejiang University, Hangzhou, Zhejiang, 310003 China
    Int J Cardiol 126:414-20. 2008
    ..The purpose of this study was to determine the ability and possible signal pathway involved of imidaprilat, an ACE inhibitor, to modulate MMP-2 and TIMP-2 in human cardiac fibroblasts in the presence of interleukin (IL)-1beta...
  93. ncbi Optical resolution of (+/-)-1,2-Bis(2-methylphenyl)ethylene-1,2-diamine as a chiral framework for 2-iminoimidazolidine with 2-methylphenyl pendant and the guanidine-catalyzed asymmetric michael reaction of tert-butyl diphenyliminoacetate and ethyl acrylat
    Akemi Ryoda
    Graduate School of Pharmaceutical Sciences, Chiba University, 1 33 Yayoi, Inage, Chiba 263 8522, Japan
    J Org Chem 73:133-41. 2008
    ..Catalysis ability of the 1,3-dimethyl-4,5-bis(2-methylphenyl)imidazolidine and the related 1,3-dibenzyl-4,5-diphenylimidazolidine was examined in the asymmetric Michael reaction of t-butyl diphenyliminoacetate and ethyl acrylate...
  94. doi Antiviral activity of pyridyl imidazolidinones against enterovirus 71 variants
    Tzu Chun Chen
    Department of Medical Biotechnology and Laboratory Science, Chang Gung University, 259 Wen Hua 1st Rd, Kwei Shan, Taoyuan, 333, Taiwan
    J Biomed Sci 15:291-300. 2008
    ..A V192M mutant was resistant to most of the derivatives, indicating that residue 192 is a key mutation for resistance to pyridyl imidazolidinone...
  95. pmc Aldose reductase inhibitor ameliorates renal vascular endothelial growth factor expression in streptozotocin-induced diabetic rats
    Joong Kyung Sung
    Department of Internal Medicine, Yonsei University Wonju College of Medicine, 162 Ilsan dong, Wonju 220 701, Korea
    Yonsei Med J 51:385-91. 2010
    ..In this study, we investigated the effects of aldose reductase inhibitor, fidarestat on diabetic nephropathy, and renal VEGF expression in a type 1 diabetic rat model...
  96. ncbi Angiotensin-converting enzyme inhibitor attenuates monocyte adhesion to vascular endothelium through modulation of intracellular zinc
    Chiari Kojima
    Life Science and Bioethics Research Center, Tokyo Medical and Dental University, 1 5 45 Yushima Bldg D 9, Bunkyo ku, Tokyo 113 8519, Japan
    J Pharmacol Exp Ther 323:855-60. 2007
    ..These data suggest that ACEI reduces MCP-1 or PMA-triggered monocyte adhesion to activated HUVECs by modulating labile zinc in monocytes. Our findings may point out a novel anti-inflammatory mechanism of ACEIs in atherogenesis...
  97. ncbi Vascular protecting effect of angiotensin receptor blocker (ARB) on the radial artery graft
    Mitsumasa Hata
    Department of Cardiovascular Surgery, Nihon University School of Medicine, Tokyo, Japan
    Ann Thorac Cardiovasc Surg 14:25-8. 2008
    ..We hypothesized that the vascular protecting effect of an angiotensin receptor blocker (ARB) reduced endothelial damage of the radial artery (RA) after coronary bypass and conducted a comparative study...
  98. ncbi Proinsecticide candidates N-(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl derivatives of imidacloprid and 1-chlorothiazolylmethyl-2-nitroimino-imidazolidine
    Ikuya Ohno
    Department of Chemistry, Faculty of Education, Gifu University, Gifu 501 1193, Japan
    Bioorg Med Chem Lett 17:4500-3. 2007
    ..4x10(-8) mol, which was similar to that for imidacloprid and the thiazolyl derivative. This result strongly suggested a regeneration of the active ingredients in vivo...
  99. ncbi Add-on blockade of (pro)renin receptor in imidapril-treated diabetic SHRsp
    Yasufumi Seki
    Department of Endocrinology and Anti Aging Medicine, Keio University School of Medicine, Tokyo, Japan
    Front Biosci (Elite Ed) 2:972-9. 2010
    ..Thus, (pro)renin receptor contributes to the accelerated pathogenesis in the heart and kidneys of diabetic SHRsp...
  100. doi Anti-tumoral activity of imidazoquines, a new class of antimalarials derived from primaquine
    Iva Fernandes
    CIQUP, Departamento de Quimica, Faculdade de Ciencias, Universidade do Porto, P 4169 007 Porto, Portugal
    Bioorg Med Chem Lett 19:6914-7. 2009
    ..Conversely, all compounds were generally inactive against HT-29, with only one of the imidazoquines having IC(50) below 50 microM. Activities against the Caco-2 cell line were modest and did not follow any defined trend...
  101. pmc Antiandrogen withdrawal in castrate-refractory prostate cancer: a Southwest Oncology Group trial (SWOG 9426)
    A Oliver Sartor
    Lank Center for Genitourinary Oncology, Dana Farber Cancer Institute, Boston, Massachusetts, USA
    Cancer 112:2393-400. 2008
    ..This study was designed to examine antiandrogen withdrawal effects within the context of a large multi-institutional prospective trial...

Research Grants91

  1. Role of poly(ADP-ribosyl)ation in diabetic neuropathy
    IRINA OBROSOVA; Fiscal Year: 2003
    ..The studies are of direct relevance to the pathogenesis of PDN and may provide the rationale for development of PARS inhibitors for its prevention and treatment. ..
  2. Na+/H+-exchanger-1 and Diabetic Neuropathy
    IRINA OBROSOVA; Fiscal Year: 2009
    ....
  3. Peroxynitrite decomposition catalyst:diabetic neuropathy
    IRINA OBROSOVA; Fiscal Year: 2006
    ..abstract_text> ..
  4. Poly(ADP-ribose) polymerase in diabetic nephropathy
    IRINA OBROSOVA; Fiscal Year: 2006
    ..abstract_text> ..
  5. 12/15-Lipoxygenase and Diabetic Neuropathy
    IRINA OBROSOVA; Fiscal Year: 2009
    ..The findings will generate new information on the role for 12/15-LO in PDN of Type 1 and Type 2 diabetes, and may provide rationale for development of 12/15-LO inhibitors for its prevention and treatment. ..
  6. 12/15-Lipoxygenase and Diabetic Neuropathy
    IRINA OBROSOVA; Fiscal Year: 2009
    ..The findings will generate new information on the role for 12/15-LO in PDN of Type 1 and Type 2 diabetes, and may provide rationale for development of 12/15-LO inhibitors for its prevention and treatment. ..
  7. Peroxynitrite, protein nitration and advanced diabetic neuropathy
    Irina G Obrosova; Fiscal Year: 2010
    ..They may also lead to identification of a new biomarker(s) of PDN with diagnostic and prognostic value. ..
  8. Na+/H+-exchanger-1 and Diabetic Neuropathy
    Irina G Obrosova; Fiscal Year: 2010
    ....
  9. 12/15-Lipoxygenase and Diabetic Neuropathy
    Irina G Obrosova; Fiscal Year: 2010
    ..The findings will generate new information on the role for 12/15-LO in PDN of Type 1 and Type 2 diabetes, and may provide rationale for development of 12/15-LO inhibitors for its prevention and treatment. ..
  10. MEASUREMENT ERRORS IN CANCER EPIDEMIOLOGY
    Bernard Rosner; Fiscal Year: 2002
    ..g., pancreatic cancer). We propose to investigate the impact of this misclassification on estimated racial differences in survival for persons with pancreatic cancer. ..
  11. ANALYSIS OF LONGITUDINAL CVD & CANCER DATA
    Bernard Rosner; Fiscal Year: 2002
    ....
  12. ALDO/KETO REDUCTASES AND DIABETIC COMPLICATIONS
    KENNETH GABBAY; Fiscal Year: 2001
    ....
  13. Amelioration of Uveitis by Aldose reductase Inhibition
    KOTA VENKATA RAMANA; Fiscal Year: 2010
    ..abstract_text> ..
  14. Chemoprevention of Colorectal Cancer by Aldose Reductase Inhibition
    Satish K Srivastava; Fiscal Year: 2010
    ..Our project will determine the mechanisms of colon carcinogenesis, and ultimately lead to the development of new chemopreventive approaches to prevent death from colon cancer. ..
  15. SYNTHESIS OF BIOLOGICALLY ACTIVE NATURAL PRODUCTS
    BARRY SNIDER; Fiscal Year: 2009
    ..In the course of these studies new methods will be developed that are of general utility for preparing drugs more economically. ..
  16. MULTIPLEX ANALYSIS OF INBORN ERRORS OF METABOLISM
    Frantisek Turecek; Fiscal Year: 2007
    ....
  17. STATISTICAL METHODS FOR OPHTHALMOLOGIC AND CLUSTER DATA
    Bernard Rosner; Fiscal Year: 2007
    ..The methods developed in this proposal as well as in the previous cycle will be available in the form of SAS macros which can be accessed at the following web site URL:(http://www.qeocities.com/bernardrosner/channina.html). ..
  18. ANALYSIS OF LONGITUDINAL CARDIOPULMONARY DATA
    Bernard Rosner; Fiscal Year: 2007
    ....
  19. Aldose Reductase: A Regulator of Inflammatory Signals
    KOTA RAMANA; Fiscal Year: 2007
    ....
  20. ANALYSIS OF LONGITUDINAL CARDIOPULMONARY DATA
    Bernard Rosner; Fiscal Year: 1990
    ..Furthermore, it is often only through the modelling of longitudinal data that processes pertaining to change can be understood...
  21. NOVEL SYNTHETIC APPROACHES TO ANTITUMOR COMPOUNDS
    BARRY TROST; Fiscal Year: 1992
    ..A strategy to one family of tumor promoters represented by teleocidin explores the concept of chemical chameleons. In most cases, the strategy also considers the problem of absolute stereochemistry...
  22. METABOLIC STUDIES IN NORMAL AND CATARACTOUS LENSES
    SATISH SRIVASTAVA; Fiscal Year: 1999
    ..abstract_text> ..
  23. MEASUREMENT ERRORS IN CANCER/RESPIRATORY EPIDEMIOLOGY
    Bernard Rosner; Fiscal Year: 1991
    ..However, issues from cancer and respiratory epidemiology are emphasized. The primary goal of this grant is to develop methods suitable for the types of studies and data most frequently encountered by investigators in these fields...
  24. METABOLIC STUDIES IN NORMAL AND CATARACTOUS LENSES
    SATISH SRIVASTAVA; Fiscal Year: 2001
    ....
  25. Determinants of Venous Thromboembolism in Older People
    Robert J Glynn; Fiscal Year: 2010
    ..Results will help identify high-risk older people, and potentially modifiable behaviors that influence risk of ..
  26. MULTIPLEX ANALYSIS OF INBORN ERRORS OF METABOLISM
    FRANTISEK contact TURECEK; Fiscal Year: 2010
    ..Technologies and procedures for the early detection of several lysosomal storage diseases are proposed in continuation of our previous successful efforts in this area. ..
  27. Determinants of Venous Thromboembolism in Older People
    Robert Glynn; Fiscal Year: 2009
    ..Results will help identify high-risk older people, and potentially modifiable behaviors that influence risk of ..
  28. Role of Aldose Reductase in Diabetic Complications
    SATISH SRIVASTAVA; Fiscal Year: 2007
    ..Our investigations will also help in evaluating the long-term risks or benefits of anti-AR therapy. ..
  29. STATISTICAL METHODS FOR OPHTHALMOLOGIC AND CLUSTER DATA
    Bernard Rosner; Fiscal Year: 2000
    ..This will allow estimation of the rates of decline of the ERG and visual field over a long period of time as well as provide estimates for an individual patient of the number of years of useful vision they can expect to have. ..
  30. SYNTHESIS OF BIOLOGICALLY ACTIVE NATURAL PRODUCTS
    BARRY SNIDER; Fiscal Year: 2001
    ..8-1.1 mg/mL. The key step in this synthesis is the intramolecular Diels-Alder reaction of trienyl glyoxylate 192 to give 191 and stereoisomers. ..
  31. ANALYSIS OF LONGITUDINAL CARDIOPULMONARY DATA
    Bernard Rosner; Fiscal Year: 1993
    ....
  32. SPECIES SUSCEPTIBILITY TO DIABETIC COMPLICATIONS
    KENNETH GABBAY; Fiscal Year: 2002
    ....
  33. Determinants of Venous Thromboembolism in Older People
    Robert Glynn; Fiscal Year: 2007
    ..Results will help identify high-risk older people, and potentially modifiable behaviors that influence risk of ..
  34. STATISTICAL METHODS FOR OPHTHALMOLOGIC AND CLUSTER DATA
    Bernard Rosner; Fiscal Year: 2004
    ..We propose to extend traditional ROC curve methods (Hanley and McNeil, 1982) to the clustered data situation where outcome on fellow eyes may be either concordant (bilateral cases) or discordant (unilateral cases). ..
  35. Neutralizing Compounds for Viral Hemorrhagic Fever
    Richard Larson; Fiscal Year: 2005
    ....
  36. Microenvironmental mechanisms of leukemia cell survival
    Richard Larson; Fiscal Year: 2009
    ..In addition, we will share this data with Dr. Tom Look at the Dana Farber Cancer Center in order to correlate his genetic findings in his T-ALL Zebra fish model with our human studies. ..
  37. SYNTHESIS OF BIOLOGICALLY ACTIVE NATURAL PRODUCTS
    BARRY SNIDER; Fiscal Year: 2007
    ..In the course of these studies new methods will be developed that are of general utility for preparing drugs more economically. ..
  38. Inflammatory cytokines in diabetic retinopathy
    Chiara Gerhardinger; Fiscal Year: 2009
    ..Recombinant IL-1ra or other anti-IL-1 drugs could become powerful tools to prevent retinopathy - with possible applications to other diabetic complications with an inflammatory component such as atherosclerosis. ..