Nicholas Bodor

Summary

Affiliation: University of Florida
Country: USA

Publications

  1. ncbi request reprint Soft drug design: general principles and recent applications
    N Bodor
    Center for Drug Discovery, University of Florida, Health Science Center, P O Box 100497, Gainesville, Florida 32610 0497, USA
    Med Res Rev 20:58-101. 2000
  2. ncbi request reprint Recent advances in retrometabolic drug design and targeting approaches
    N Bodor
    Center for Drug Discovery, University of Florida, Gainesville, USA
    Pharmazie 55:163-6. 2000
  3. ncbi request reprint Design, pharmacokinetic, and pharmacodynamic evaluation of a new class of soft anticholinergics
    Fenglei Huang
    Center for Drug Discovery, College of Pharmacy, University of Florida, Gainesville, Florida 32610, USA
    Pharm Res 20:1681-9. 2003
  4. ncbi request reprint Targeting drugs to the brain by redox chemical delivery systems
    L Prokai
    Center for Drug Discovery, College of Pharmacy, University of Florida, J Hillis Miller Health Center, Gainesville, FL 32610, USA
    Med Res Rev 20:367-416. 2000
  5. ncbi request reprint Novel, cell-penetrating molecular transporters with flexible backbones and permanently charged side-chains
    N Bodor
    Center for Drug Discovery, University of Florida, Gainesville, FL 32610 0497, USA
    J Pharm Pharmacol 59:1065-76. 2007
  6. ncbi request reprint Corticosteroid design for the treatment of asthma: structural insights and the therapeutic potential of soft corticosteroids
    Nicholas Bodor
    IVAX Research, Inc, Miami, Florida, USA
    Curr Pharm Des 12:3241-60. 2006
  7. ncbi request reprint Effect of cyclodextrins on the solubility and stability of a novel soft corticosteroid, loteprednol etabonate
    N Bodor
    Center for Drug Discovery, College of Pharmacy, University of Florida, Gainesville, USA
    Pharmazie 55:206-9. 2000
  8. ncbi request reprint Synthesis and pharmacological evaluation of prodrugs of valproic acid
    N Bodor
    Center for Drug Discovery, University of Florida, Gainesville, USA
    Pharmazie 55:184-6. 2000
  9. pmc Ophthalmic drug design based on the metabolic activity of the eye: soft drugs and chemical delivery systems
    Nicholas Bodor
    Center for Drug Discovery, University of Florida, Health Science Center, PO Box 100497, Gainesville, FL 32610 0497, USA
    AAPS J 7:E820-33. 2005
  10. ncbi request reprint Pharmacokinetic and pharmacodynamic evaluations of the zwitterionic metabolite of a new series of N-substituted soft anticholinergics
    Whei Mei Wu
    Center for Drug Discovery, College of Pharmacy, University of Florida, Gainesville, Florida, USA
    Pharm Res 22:2035-44. 2005

Collaborators

Detail Information

Publications41

  1. ncbi request reprint Soft drug design: general principles and recent applications
    N Bodor
    Center for Drug Discovery, University of Florida, Health Science Center, P O Box 100497, Gainesville, Florida 32610 0497, USA
    Med Res Rev 20:58-101. 2000
    ..Whenever possible, pharmacokinetic and pharmacodynamic properties are briefly summarized and compared to those of other compounds used in the same field...
  2. ncbi request reprint Recent advances in retrometabolic drug design and targeting approaches
    N Bodor
    Center for Drug Discovery, University of Florida, Gainesville, USA
    Pharmazie 55:163-6. 2000
    ..For the chemical delivery system (CDS) approach, the latest advances achieved in the brain targeting of peptides such as kyotorphin and TRH analogues are described...
  3. ncbi request reprint Design, pharmacokinetic, and pharmacodynamic evaluation of a new class of soft anticholinergics
    Fenglei Huang
    Center for Drug Discovery, College of Pharmacy, University of Florida, Gainesville, Florida 32610, USA
    Pharm Res 20:1681-9. 2003
    ..To design and evaluate a new class of soft anticholinergics with subtype selectivity...
  4. ncbi request reprint Targeting drugs to the brain by redox chemical delivery systems
    L Prokai
    Center for Drug Discovery, College of Pharmacy, University of Florida, J Hillis Miller Health Center, Gainesville, FL 32610, USA
    Med Res Rev 20:367-416. 2000
    ..The investigations accentuate the need for considering physicochemical, metabolic, and pharmacokinetic properties in designing of carrier systems that are able to target drugs into the central nervous system...
  5. ncbi request reprint Novel, cell-penetrating molecular transporters with flexible backbones and permanently charged side-chains
    N Bodor
    Center for Drug Discovery, University of Florida, Gainesville, FL 32610 0497, USA
    J Pharm Pharmacol 59:1065-76. 2007
    ..g., Arg(+), Lys(+)). A nonamer analogue showed transporter activity resulting in increased cellular uptake in human carcinoma (HeLa) cells...
  6. ncbi request reprint Corticosteroid design for the treatment of asthma: structural insights and the therapeutic potential of soft corticosteroids
    Nicholas Bodor
    IVAX Research, Inc, Miami, Florida, USA
    Curr Pharm Des 12:3241-60. 2006
    ....
  7. ncbi request reprint Effect of cyclodextrins on the solubility and stability of a novel soft corticosteroid, loteprednol etabonate
    N Bodor
    Center for Drug Discovery, College of Pharmacy, University of Florida, Gainesville, USA
    Pharmazie 55:206-9. 2000
    ..The exothermic peak found in the DSC diagram with LE/DMCD sample, but not with LE/HPBCD samples, suggests a stronger complex formed between LE and DMCD, resulting in higher solubility and stability of LE in DMCD than in HPBCD...
  8. ncbi request reprint Synthesis and pharmacological evaluation of prodrugs of valproic acid
    N Bodor
    Center for Drug Discovery, University of Florida, Gainesville, USA
    Pharmazie 55:184-6. 2000
    ..The anticonvulsant activity of the compound 7 (MES test) expressed as ED50 is four times higher than that reported for valproic acid...
  9. pmc Ophthalmic drug design based on the metabolic activity of the eye: soft drugs and chemical delivery systems
    Nicholas Bodor
    Center for Drug Discovery, University of Florida, Health Science Center, PO Box 100497, Gainesville, FL 32610 0497, USA
    AAPS J 7:E820-33. 2005
    ....
  10. ncbi request reprint Pharmacokinetic and pharmacodynamic evaluations of the zwitterionic metabolite of a new series of N-substituted soft anticholinergics
    Whei Mei Wu
    Center for Drug Discovery, College of Pharmacy, University of Florida, Gainesville, Florida, USA
    Pharm Res 22:2035-44. 2005
    ..This study was conducted to evaluate the zwitterionic common metabolite of a novel series of N-substituted soft analogs of glycopyrrolate both as racemates and as 2R isomers...
  11. ncbi request reprint Designing safer (soft) drugs by avoiding the formation of toxic and oxidative metabolites
    Nicholas Bodor
    IVAX Research Inc, 4400 Biscayne Boulecard, Miami, FL 33137, USA
    Mol Biotechnol 26:123-32. 2004
    ..Design principles for various soft drug classes are briefly summarized together with computerized tools intended to make the application of these principles more quantitative and more accessible...
  12. doi request reprint Pharmacokinetics of the sequential metabolites of loteprednol etabonate in rats
    Whei Mei Wu
    Center for Drug Discovery, College of Pharmacy, University of Florida, Gainesville, FL 32610 0497, USA
    J Pharm Pharmacol 60:291-7. 2008
    ..In a manner similar to that seen for LE, dose-dependent elimination was observed both in AE and A. These results suggested that both AE and A were ideal leads for the design of soft steroids based on the inactive metabolite approach...
  13. ncbi request reprint Soft quaternary anticholinergics: comprehensive quantitative structure-activity relationship (QSAR) with a linearized biexponential (LinBiExp) model
    Peter Buchwald
    IVAX Research, Inc, 4400 Biscayne Boulevard, Miami, FL 33137, USA
    J Med Chem 49:883-91. 2006
    ....
  14. ncbi request reprint In vitro and in vivo evaluations of dihydroquinoline- and dihydroisoquinoline-based targetor moieties for brain-specific chemical delivery systems
    Nicholas Bodor
    Center for Drug Discovery, University of Florida, Health Science Center, Gainesville 32610 0497, USA
    J Drug Target 10:63-71. 2002
    ....
  15. ncbi request reprint Synthesis and biological evaluations of brain-targeted chemical delivery systems of [Nva2]-TRH
    Jiaxiang Wu
    Center for Drug Discovery, College of Pharmacy, University of Florida, Gainesville 32611, USA
    J Pharm Pharmacol 54:945-50. 2002
    ..The results indicate that the fully packaged delivery system is necessary to produce the successful brain targeting of the precursor construct and effective release of the Gln-Nva-ProNH2...
  16. ncbi request reprint Effect of 2-hydroxypropyl-beta-cyclodextrin on the solubility, stability, and pharmacological activity of the chemical delivery system of TRH analogs
    W M Wu
    Center for Drug Discovery, University of Florida, Gainesville, FL, USA
    Pharmazie 57:130-4. 2002
    ..These results demonstrate the usefulness of cyclodextrin in the formulation of the CDSs of TRH analogs...
  17. ncbi request reprint Estrogens may reduce mortality and ischemic damage caused by middle cerebral artery occlusion in the female rat
    J W Simpkins
    Department of Pharmacodynamics and the Center for the Neurobiology of Aging, College of Pharmacy, University of Florida, Gainesville 32610, USA
    J Neurosurg 87:724-30. 1997
    ....
  18. ncbi request reprint Recent advances in retrometabolic design approaches
    N Bodor
    Center for Drug Discovery, University of Florida, P O Box 100497, JHMHC, Gainesville, FL 32610, USA
    J Control Release 62:209-22. 1999
    ..Most recent advances involve FDA approval of a soft steroid, as well as the first successful brain targeting of various neuropeptides and their brain-targeted analogs...
  19. ncbi request reprint Barriers to remember: brain-targeting chemical delivery systems and Alzheimer's disease
    Nicholas Bodor
    IVAX Research, 4400 Biscayne Boulevard, Miami, FL 33137, USA
    Drug Discov Today 7:766-74. 2002
    ..Many potential therapeutic applications can be envisioned for such CDSs; here, the potential of brain-targeted estradiol for the prevention and treatment of Alzheimer's disease is reviewed in detail...
  20. ncbi request reprint Unified pharmacogenetics-based parent-metabolite pharmacokinetic model incorporating acetylation polymorphism for talampanel in humans
    Peter Buchwald
    IVAX Research, Inc, 4400 Biscayne Boulevard, Miami, FL 33137, USA
    J Pharmacokinet Pharmacodyn 32:377-400. 2005
    ..Such PK models can provide quantitative estimates of relative in vivo metabolism rates for routes catalyzed by functionally polymorphic enzymes...
  21. ncbi request reprint Designing safer (soft) drugs by avoiding the formation of toxic and oxidative metabolites
    Nicholas Bodor
    Department of Pharmaceutics, Center for Drug Discovery, University of Florida, College of Pharmacy, Gainesville, FL, USA
    Methods Mol Biol 186:301-12. 2002
  22. ncbi request reprint Soft drugs--10. Blanching activity and receptor binding affinity of a new type of glucocorticoid: loteprednol etabonate
    P Druzgala
    Center for Drug Discovery, University of Florida, Gainesville
    J Steroid Biochem Mol Biol 38:149-54. 1991
    ..The results showed that loteprednol etabonate has good skin-permeation properties and strong glucocorticoid activity...
  23. ncbi request reprint Synthesis and pharmacological effects of new, N-substituted soft anticholinergics based on glycopyrrolate
    F Ji
    Center for Drug Discovery, College of Pharmacy, University of Florida, PO Box 100497, Gainesville, FL 32610 0497, USA
    J Pharm Pharmacol 57:1427-35. 2005
    ....
  24. ncbi request reprint Soft drugs. 21. Design and evaluation of soft analogs of propantheline
    G Brouillette
    Center for Drug Discovery, University of Florida, Gainesville 32610, USA
    J Pharm Sci 85:619-23. 1996
    ..The equipotency of this soft analog coupled with increased metabolic lability proves the rationality of the soft drug approach for the design of safer therapeutic agents with higher therapeutic indices...
  25. ncbi request reprint Physicochemical aspects of the enzymatic hydrolysis of carboxylic esters
    P Buchwald
    IVAX Research, Inc, Miami, Florida, USA
    Pharmazie 57:87-93. 2002
    ..Available in vitro human blood data suggest that shortest half-lives are achieved with sterically non-hindered chains that are neither too short nor too long and are of around four carbon-atom long...
  26. ncbi request reprint Soft corticosteroids for local immunosuppression: exploring the possibility for the use of loteprednol etabonate for islet transplantation
    N Bocca
    Diabetes Research Institute, Miller School of Medicine, University of Miami, Miami, FL 33136, USA
    Pharmazie 63:226-32. 2008
    ....
  27. ncbi request reprint Pharmacokinetics and delta1-cortienic acid excretion after intravenous administration of prednisolone and loteprednol etabonate in rats
    W M Wu
    Center for Drug Discovery College of Pharmacy, University of Florida, Gainesville 32610 0497, USA
    Pharmazie 65:412-6. 2010
    ..11 +/- 0.03% in bile and 0.22 +/- 0.04% in urine) indicating that the presence of the delta1 double bond (delta1-unsaturation) does not affect significantly this metabolic conversion...
  28. ncbi request reprint Feasibility of localized immunosuppression: 2. PLA microspheres for the sustained local delivery of a soft immunosuppressant
    E Pinto
    Department of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA
    Pharmazie 65:429-35. 2010
    ..However, further confirmation is required before use in cell or organ transplantation...
  29. ncbi request reprint Stereoisomers of N-substituted soft anticholinergics and their zwitterionic metabolite based on glycopyrrolate--syntheses and pharmacological evaluations
    W M Wu
    Center for Drug Discovery, College of Pharmacy, University of Florida, Gainesville, FL 32610 0497, USA
    Pharmazie 63:200-9. 2008
    ..H) [3'-(2-cyclopentyl-2-phenyl-2-hydroxyacetoxy)-1'-methyl-1'-carboxymethylpyrrolidinium inner salt] were synthesized and their pharmacological activities were evaluated in vitro and in vivo...
  30. ncbi request reprint Feasibility of localized immunosuppression: 1. Exploratory studies with glucocorticoids in a biohybrid device designed for cell transplantation
    P Buchwald
    Diabetes Research Institute, Miller School of Medicine, University of Miami, Miami, FL 33136, USA
    Pharmazie 65:421-8. 2010
    ....
  31. ncbi request reprint Recent advances in retrometabolic drug design (RMDD) and development
    N Bodor
    Center for Drug Discovery, University of Florida, Gainesville, FL 32610 0497, USA
    Pharmazie 65:395-403. 2010
    ....
  32. ncbi request reprint Regioselective O-alkylation of cortienic acid and synthesis of a new class of glucocorticoids containing a 17 alpha-alkoxy, a 17 alpha-(1'-alkoxyethyloxy), a 17 alpha-alkoxymethyloxy, or a 17 alpha-methylthiomethyloxy function
    P Druzgala
    Center for Drug Discovery, University of Florida, Gainesville 32610
    Steroids 56:490-4. 1991
    ..A 17 alpha-alkoxy function is a new feature in cortisol analogs...
  33. ncbi request reprint Studies on a soft glycopyrrolate analog, SG-1
    F Ji
    Center for Drug Discovery, University of Florida, Gainesville, Florida, USA
    Pharmazie 57:138-41. 2002
    ..35 min, respectively. In human plasma and blood, half-lives were 19.93 and 88.32 min, respectively. SG-1 was relatively stable under acidic conditions (pH 5 and lower). SG-1 is a promising, clinically useful short acting anticholinergic...
  34. ncbi request reprint A simple, predictive, structure-based skin permeability model
    P Buchwald
    Center for Drug Discovery, University of Florida, Gainesville 32610-0497, USA
    J Pharm Pharmacol 53:1087-98. 2001
    ..As the new model is structure based and fully computerized, it allows direct estimation of skin permeability for any molecule of known structure without the need to obtain octanol-water partition coefficients or other experimental data...
  35. ncbi request reprint Retrometabolic drug design--novel aspects, future directions
    N Bodor
    IVAX Corporation, Miami, Florida, USA
    Pharmazie 56:S67-74. 2001
    ....
  36. ncbi request reprint Soft glucocorticoid design: structural elements and physicochemical parameters determining receptor-binding affinity
    P Buchwald
    IVAX, Miami, Florida 33137, USA
    Pharmazie 59:396-404. 2004
    ..According to these data, receptor binding affinity at the GR is dramatically increased by 6alpha- or 9alpha-halogenation and it also tends to increase with increasing lipophilicity...
  37. ncbi request reprint Soft cannabinoid analogues as potential anti-glaucoma agents
    A Buchwald
    Center for Drug Discovery, College of Pharmacy, University of Florida, Gainesville, Florida, USA
    Pharmazie 57:108-14. 2002
    ..The preliminary i.v. experimental data could be successfully described by an indirect response PK/PD model...
  38. ncbi request reprint Design, pharmacokinetic, and pharmacodynamic evaluation of soft anticholinergics based on tropyl alpha-phenylcyclopentylacetate
    F Huang
    Center for Drug Discovery, College of Pharmacy, University of Florida, USA
    Pharmazie 57:115-21. 2002
    ..In vitro and in vivo pharmacokinetic studies demonstrated that the soft anticholinergics were rapidly hydrolyzed into the corresponding inactive metabolites once they were introduced into the systemic circulation...
  39. pmc Receptor binding studies of soft anticholinergic agents
    F Huang
    Center for Drug Discovery, College of Pharmacy, University of Florida, Gainesville, FL 32610-0497, USA
    AAPS PharmSci 3:E30. 2001
    ..A linear regression equation using ovality (O(e)), dipole moment (D), and a calculated log octanol-water partition coefficient (QLogP) gave reasonably good descriptions (r = 0.88) for the pK(i) (m3) values...
  40. ncbi request reprint Pharmacological effects of some newly developed soft anticholinergics and a receptor-binding QSAR study
    N Mori
    Center for Drug Discovery, College of Pharmacy, University of Florida, Florida 32610 0497, USA
    Pharmazie 61:148-53. 2006
    ....
  41. ncbi request reprint Potency and specificity of the pharmacological action of a new, antiasthmatic, topically administered soft steroid, etiprednol dicloacetate (BNP-166)
    Istvan Kurucz
    Department of Immunopharmacology, IVAX Drug Research Institute, Budapest, Hungary
    J Pharmacol Exp Ther 307:83-92. 2003
    ..These data indicate that the strong local effect of the compound will very likely be accompanied with a significantly reduced systemic activity predicting favorable selectivity in the pharmacological action of etiprednol dicloacetate...