Genomes and Genes
Summary: Substituted derivatives of hydrazine (formula H2N-NH2).
- Abdel Aal M, El Sayed W, El Kosy S, El Ashry E. Synthesis and antiviral evaluation of novel 5-(N-Aryl-aminomethyl-1,3,4-oxadiazol-2-yl)hydrazines and their sugars, 1,2,4-triazoles, tetrazoles and pyrazolyl derivatives. Arch Pharm (Weinheim). 2008;341:307-13 pubmed publisher..The results revealed that the sugar hydrazones 6a,b showed higher antiviral activity compared to the other hydrazones and their acetylated derivatives. ..
- Su L, Cheng C, Mruk D. Adjudin-mediated Sertoli-germ cell junction disassembly affects Sertoli cell barrier function in vitro and in vivo. Int J Biochem Cell Biol. 2010;42:1864-75 pubmed publisher..These results illustrate that a unique mechanism exists to maintain blood-testis barrier integrity at all costs, irrespective of the presence of germ cells in the seminiferous epithelium of the testis. ..
- Cheng G, Saleh M, Marcher C, Vasey S, Mayer B, Aivado M, et al. Eltrombopag for management of chronic immune thrombocytopenia (RAISE): a 6-month, randomised, phase 3 study. Lancet. 2011;377:393-402 pubmed publisher..These benefits should be balanced with the potential risks associated with eltrombopag treatment. GlaxoSmithKline. ..
- Stasi R, Evangelista M, Amadori S. Novel thrombopoietic agents: a review of their use in idiopathic thrombocytopenic purpura. Drugs. 2008;68:901-12 pubmed..Ongoing phase III clinical trials will reveal the potential of these agents in the management of ITP prior to splenectomy and for long-term maintenance therapy, as well as their relative benefit compared with standard of care treatment. ..
- Dahlgren M, Zetterström C, Gylfe S, Linusson A, Elofsson M. Statistical molecular design of a focused salicylidene acylhydrazide library and multivariate QSAR of inhibition of type III secretion in the Gram-negative bacterium Yersinia. Bioorg Med Chem. 2010;18:2686-703 pubmed publisher..Y. pseudotuberculosis and C. trachomatis cell-based infection models showed that compounds identified in this study are selective and non-toxic inhibitors of T3S dependent virulence...
- Erickson Miller C, Kirchner J, Aivado M, May R, Payne P, Chadderton A. Reduced proliferation of non-megakaryocytic acute myelogenous leukemia and other leukemia and lymphoma cell lines in response to eltrombopag. Leuk Res. 2010;34:1224-31 pubmed publisher..The decrease in proliferation appears to be through a TpoR-independent, nonapoptotic mechanism. These findings suggest that eltrombopag does not enhance, but rather inhibits, proliferation of leukemia cell lines in vitro. ..
- Slepenkin A, Chu H, Elofsson M, Keyser P, Peterson E. Protection of mice from a Chlamydia trachomatis vaginal infection using a Salicylidene acylhydrazide, a potential microbicide. J Infect Dis. 2011;204:1313-20 pubmed publisher..05). The quantity of IFUs shed and antibody titers to Chlamydia were significantly higher for the control group (P < .05). In summary, INP0341 is a promising compound to be considered for formulation as a vaginal microbicide. ..
- Will B, Kawahara M, Luciano J, Bruns I, Parekh S, Erickson Miller C, et al. Effect of the nonpeptide thrombopoietin receptor agonist Eltrombopag on bone marrow cells from patients with acute myeloid leukemia and myelodysplastic syndrome. Blood. 2009;114:3899-908 pubmed publisher..These results provide a preclinical rationale for further testing of Eltrombopag for treatment of thrombocytopenia in AML and MDS. ..
- Zhen G, Kim Y, Li R, Yocum J, Kapoor N, Langer J, et al. PGE2 EP1 receptor exacerbated neurotoxicity in a mouse model of cerebral ischemia and Alzheimer's disease. Neurobiol Aging. 2012;33:2215-9 pubmed publisher..Exploring potential therapeutic agent targeting EP1 receptor could potentially benefit treatments for stroke and AD patients. ..
- Chu H, Slepenkin A, Elofsson M, Keyser P, de la Maza L, Peterson E. Candidate vaginal microbicides with activity against Chlamydia trachomatis and Neisseriagonorrhoeae. Int J Antimicrob Agents. 2010;36:145-50 pubmed publisher..trachomatis, are not cytotoxic and do not inhibit organisms that compose the normal vaginal flora. ..
- Liu X, Xu J, Dong F, Li Y, Song W, Zheng Y. Residue analysis of four diacylhydrazine insecticides in fruits and vegetables by Quick, Easy, Cheap, Effective, Rugged, and Safe (QuEChERS) method using ultra-performance liquid chromatography coupled to tandem mass spectrometry. Anal Bioanal Chem. 2011;401:1051-8 pubmed publisher..5% with RSDs in the range of 1.4-13.8% (n = 5) for all analytes. This study provides a theoretical basis for China to draw up maximum residue limits and analytical method for diacylhydrazine insecticide in vegetables and fruits. ..
- Giannini E, Savarino V. Thrombocytopenia in liver disease. Curr Opin Hematol. 2008;15:473-80 pubmed publisher..In these patients, novel therapies for treating thrombocytopenia seem promising, although it remains to be established whether treating thrombocytopenia may help improve liver disease-associated coagulopathy. ..
- Vadhan Raj S. Management of chemotherapy-induced thrombocytopenia: current status of thrombopoietic agents. Semin Hematol. 2009;46:S26-32 pubmed publisher..The clinical trials of romiplostim and eltrombopag are currently ongoing to optimize their dose and schedule in ameliorating chemotherapy-induced thrombocytopenia. ..
- Castanedo G, Seng P, Blaquiere N, Trapp S, Staben S. Rapid synthesis of 1,3,5-substituted 1,2,4-triazoles from carboxylic acids, amidines, and hydrazines. J Org Chem. 2011;76:1177-9 pubmed publisher..1,3,5-trisubstituted 1,2,4-triazoles has been developed from reaction of carboxylic acids, primary amidines, and monosubstituted hydrazines. This highly regioselective and one-pot process provides rapid access to highly diverse triazoles.
- Erickson Miller C, DeLorme E, Tian S, Hopson C, Landis A, Valoret E, et al. Preclinical activity of eltrombopag (SB-497115), an oral, nonpeptide thrombopoietin receptor agonist. Stem Cells. 2009;27:424-30 pubmed publisher..These results suggest that eltrombopag and Tpo may be able to act additively to increase platelet production. ..
- Fischborn S, Soerensen J, Potschka H. Targeting the prostaglandin E2 EP1 receptor and cyclooxygenase-2 in the amygdala kindling model in mice. Epilepsy Res. 2010;91:57-65 pubmed publisher..The contrasting impact of the EP1 receptor antagonist and agonist suggests that EP1 receptors can influence endogenous mechanisms involved in termination of seizure activity. ..
- Liu X, Pan L, Ma Y, Weng J, Tan C, Li Y, et al. Design, synthesis, biological activities, and 3D-QSAR of new N,N'-diacylhydrazines containing 2-(2,4-dichlorophenoxy)propane moiety. Chem Biol Drug Des. 2011;78:689-94 pubmed publisher..7%) at 1500 g/ha, although it is less active than 2,4-D. Meanwhile, this compound also exhibited good fungicidal activity against C. orbiculare (Berk aLMont) Arx (82.16%). ..
- Dahlgren M, Oberg C, Wallin E, Janson P, Elofsson M. Synthesis of 2-(2-aminopyrimidine)-2,2-difluoroethanols as potential bioisosters of salicylidene acylhydrazides. Molecules. 2010;15:4423-38 pubmed publisher..The synthesis of a library of 2-(2-amino-pyrimidine)-2,2-difluoro-ethanols is described in this paper. ..
- Bussel J, Provan D, Shamsi T, Cheng G, Psaila B, Kovaleva L, et al. Effect of eltrombopag on platelet counts and bleeding during treatment of chronic idiopathic thrombocytopenic purpura: a randomised, double-blind, placebo-controlled trial. Lancet. 2009;373:641-8 pubmed publisher..Eltrombopag is an effective treatment for managment of thrombocytopenia in chronic ITP. ..
- O Day S, Gonzalez R, Lawson D, Weber R, Hutchins L, Anderson C, et al. Phase II, randomized, controlled, double-blinded trial of weekly elesclomol plus paclitaxel versus paclitaxel alone for stage IV metastatic melanoma. J Clin Oncol. 2009;27:5452-8 pubmed publisher..A multinational, phase III trial (SYMMETRY) of E + P compared with paclitaxel alone in metastatic melanoma has closed. ..
- Vizcaíno G, Diez Ewald M, Vizcaíno Carruyo J. [Treatment of chronic immune thrombocytopenic purpura. Looking for something better. Review]. Invest Clin. 2009;50:95-108 pubmed..It is obvious that the cost-benefit from the different treatments is inclined towards those of lower cost and minimal secondary effects. ..
- Kirshner J, He S, Balasubramanyam V, Kepros J, Yang C, Zhang M, et al. Elesclomol induces cancer cell apoptosis through oxidative stress. Mol Cancer Ther. 2008;7:2319-27 pubmed publisher..Thus, the induction of oxidative stress by elesclomol exploits this unique characteristic of cancer cells by increasing ROS levels beyond a threshold that triggers cell death. ..
- Wang D, Zetterström C, Gabrielsen M, Beckham K, Tree J, Macdonald S, et al. Identification of bacterial target proteins for the salicylidene acylhydrazide class of virulence-blocking compounds. J Biol Chem. 2011;286:29922-31 pubmed publisher..We also examine the contribution of selected target proteins to the pathogenicity of Yersinia pseudotuberculosis and to expression of virulence genes in Escherichia coli O157. ..
- Williams D, Peng B, Bailey C, Wire M, Deng Y, Park J, et al. Effects of food and antacids on the pharmacokinetics of eltrombopag in healthy adult subjects: two single-dose, open-label, randomized-sequence, crossover studies. Clin Ther. 2009;31:764-76 pubmed publisher..A single dose of eltrombopag was generally well tolerated in these healthy volunteers. ..
- Nurden A, Viallard J, Nurden P. New-generation drugs that stimulate platelet production in chronic immune thrombocytopenic purpura. Lancet. 2009;373:1562-9 pubmed publisher..However, long-term side-effects are being assessed and the exact role of these agents in the overall treatment strategy of chronic idiopathic thrombocytopenic purpura remains to be established. ..
- Zhao Q, Shang J, Huang Z, Wang K, Bi F, Huang R, et al. Synthesis and insecticidal activities of novel N-sulfenyl-N'-tert-butyl-N,N'-diacylhydrazines. 2. N-substituted phenoxysulfenate derivatives. J Agric Food Chem. 2008;56:5254-9 pubmed publisher..Furthermore, the compound IIIi exhibits higher contact activities against Asian corn borer, tobacco cutworm, and cotton bollworm than RH-5992. ..
- Schmid M, Hooper A, Klotz M, Woebken D, Lam P, Kuypers M, et al. Environmental detection of octahaem cytochrome c hydroxylamine/hydrazine oxidoreductase genes of aerobic and anaerobic ammonium-oxidizing bacteria. Environ Microbiol. 2008;10:3140-9 pubmed publisher..We propose that OCC protein-encoding genes are suitable targets for molecular ecological studies on both aerobic and anaerobic ammonium-oxidizing bacteria...
- Abe T, Kunz A, Shimamura M, Zhou P, Anrather J, Iadecola C. The neuroprotective effect of prostaglandin E2 EP1 receptor inhibition has a wide therapeutic window, is sustained in time and is not sexually dimorphic. J Cereb Blood Flow Metab. 2009;29:66-72 pubmed publisher..The data provide proof of principle that EP1 receptor inhibition is a potentially valuable strategy for neuroprotection that deserves further preclinical investigation for therapeutic application in human stroke. ..
- Xiao X, Mruk D, Lee W, Cheng C. c-Yes regulates cell adhesion at the blood-testis barrier and the apical ectoplasmic specialization in the seminiferous epithelium of rat testes. Int J Biochem Cell Biol. 2011;43:651-65 pubmed publisher..In summary, c-Yes regulates BTB and apical ES integrity by maintaining proper distribution of integral membrane proteins and actin filament organization at these sites...
- Zaharia V, Ignat A, Palibroda N, Ngameni B, Kuete V, Fokunang C, et al. Synthesis of some p-toluenesulfonyl-hydrazinothiazoles and hydrazino-bis-thiazoles and their anticancer activity. Eur J Med Chem. 2010;45:5080-5 pubmed publisher..Compounds 2a, 2c, 2d, 2e and 3a showed significant anticancer activities (IC(50)<10 ?M) on both prostate DU-145 and hepatocarcinoma Hep-G2 cancer cell lines. ..
- Kellum A, Jagiello Gruszfeld A, Bondarenko I, Patwardhan R, Messam C, Mostafa Kamel Y. A randomized, double-blind, placebo-controlled, dose ranging study to assess the efficacy and safety of eltrombopag in patients receiving carboplatin/paclitaxel for advanced solid tumors. Curr Med Res Opin. 2010;26:2339-46 pubmed publisher..Further investigation is needed to identify the optimal dose(s) and schedule of eltrombopag in patients receiving myelosuppressive chemotherapy. ..
- Gudmundsdottir A, Paul C, Nitz M. Stability studies of hydrazide and hydroxylamine-based glycoconjugates in aqueous solution. Carbohydr Res. 2009;344:278-84 pubmed publisher..All the compounds were increasingly stable as the pH approached neutrality. Conjugate hydrolysis rates mirrored those found for O-glycoside hydrolysis where conjugates formed from electron-rich monosaccharides hydrolyzed more rapidly. ..
- Wu L, Zhou L, Liu D, Vogt F, Kord A. LC-MS/MS and density functional theory study of copper(II) and nickel(II) chelating complexes of elesclomol (a novel anticancer agent). J Pharm Biomed Anal. 2011;54:331-6 pubmed publisher..25 kcal/mol). This relative stability of the chelating complexes of elesclomol is consistent with the Irving-Williams series of bindings to ligands. ..
- Chen H, Ahsan S, Santiago Berrios M, Abruña H, Webb W. Mechanisms of quenching of Alexa fluorophores by natural amino acids. J Am Chem Soc. 2010;132:7244-5 pubmed publisher..In light of this finding, the potential effect of intramolecular quenching should be considered in the interpretation of data that involves quantitative measurements of fluorescence intensity in proteins. ..
- ..Eltrombopag was generally well tolerated in clinical trials, with an adverse events profile that did not differ significantly from that with placebo. ..
- Pinto J, Silva V, Silva A, Claramunt R, Sanz D, Torralba M, et al. The structure of azines derived from C-formyl-1H-imidazoles in solution and in the solid state: tautomerism, configurational and conformational studies. Magn Reson Chem. 2013;51:203-21 pubmed publisher..The configuration around the central C = N bonds has been determined and some insights about prototropic tautomerism and conformation have been gained. ..
- Barnes R, Bandi R, Wong W, Barraud N, McDougald D, Fane A, et al. Optimal dosing regimen of nitric oxide donor compounds for the reduction of Pseudomonas aeruginosa biofilm and isolates from wastewater membranes. Biofouling. 2013;29:203-12 pubmed publisher..The data present strong evidence for the application of these NO donor compounds for prevention of biofouling in an industrial setting. ..
- Karimi Maleh H, Moazampour M, Ensafi A, Mallakpour S, Hatami M. An electrochemical nanocomposite modified carbon paste electrode as a sensor for simultaneous determination of hydrazine and phenol in water and wastewater samples. Environ Sci Pollut Res Int. 2014;21:5879-88 pubmed publisher..0 nmol L(-1). SWV was used for simultaneous determination of hydrazine and phenol at the modified electrode and quantitation of hydrazine and phenol in some real samples by the standard addition method. ..
- Cihan ÃœstÃ¼ndaÄŸ G, Åžatana D, Ã–zhan G, Ã‡apan G. Indole-based hydrazide-hydrazones and 4-thiazolidinones: synthesis and evaluation as antitubercular and anticancer agents. J Enzyme Inhib Med Chem. 2016;31:369-80 pubmed publisher..Compound 6b showed an interesting anticancer profile against different human tumor-derived cell lines at sub-micromolar concentrations with obvious selectivity toward colon cancer cell line COLO 205. ..
- Popiołek Ł, Biernasiuk A. New Hydrazides and Hydrazide-Hydrazones of 2,3-Dihalogen Substituted Propionic Acids: Synthesis and in vitro Antimicrobial Activity Evaluation. Chem Biodivers. 2017;14: pubmed publisher..All obtained compounds were identified on the basis of spectral methods (1 H-NMR, 13 C-NMR) and in vitro screened against a panel of bacterial and fungal strains according to EUCAST and CLSI guidelines. ..
- ÅženkardeÅŸ S, Kaushik Basu N, Durmaz Ä, Manvar D, Basu A, Atalay R, et al. Synthesis of novel diflunisal hydrazide-hydrazones as anti-hepatitis C virus agents and hepatocellular carcinoma inhibitors. Eur J Med Chem. 2016;108:301-308 pubmed publisher..34 16.21 4.74, 9.29 and 8.33Â Î¼M for Huh7, HepG2, Hep3B, Mahlavu, FOCUS and SNU-475Â cells, respectively, and produced dramatic cell cycle arrest at SubG1/G0 phase as an indicator of apoptotic cell death induction. ..
- Matveychuk D, Nunes E, Ullah N, Velazquez Martinez C, MacKenzie E, Baker G. Comparison of phenelzine and geometric isomers of its active metabolite, ?-phenylethylidenehydrazine, on rat brain levels of amino acids, biogenic amine neurotransmitters and methylamine. J Neural Transm (Vienna). 2013;120:987-96 pubmed publisher..All three drugs significantly increased rat brain levels of methylamine, with (E)- and (Z)-PEH causing a greater increase than phenelzine. These results are discussed in relation to the possible therapeutic applications of these drugs. ..
- Paolino D, Licciardi M, Celia C, Giammona G, Fresta M, Cavallaro G. Folate-targeted supramolecular vesicular aggregates as a new frontier for effective anticancer treatment in in vivo model. Eur J Pharm Biopharm. 2012;82:94-102 pubmed publisher..The obtained data showed that supramolecular systems could represent an innovative drug delivery system by self-assembling liposomes and biocompatible polymers to be potentially used for anticancer treatment. ..
- Johnson G, Chozinski T, Salmon D, Moghaddam A, Chen H, Miranda K. Quantitative detection of nitroxyl upon trapping with glutathione and labeling with a specific fluorogenic reagent. Free Radic Biol Med. 2013;63:476-84 pubmed publisher..This suggests that GS(O)NH?, which is a selective biomarker of HNO, may be produced in concentrations that are amenable to in vivo analysis. ..
- Ray Banerjee S, Pullambhatla M, Foss C, Falk A, Byun Y, Nimmagadda S, et al. Effect of chelators on the pharmacokinetics of (99m)Tc-labeled imaging agents for the prostate-specific membrane antigen (PSMA). J Med Chem. 2013;56:6108-21 pubmed publisher..These results suggest that choice of chelator is an important pharmacokinetic consideration in the development of (99m)Tc-labeled radiopharmaceuticals targeting PSMA. ..
- Shahidi L, Taei M, Banitaba S, Tavakkoli N. A new 2-amino-3-pynanopyrane-3- carbonitrile derivative for electrocatalytic oxidation and determination of hydrazine. Mater Sci Eng C Mater Biol Appl. 2017;75:1154-1160 pubmed publisher..Finally, the fabricated sensor was agreeably utilized for the determination of hydrazine in real samples. ..