Search

Your search keyword '"GAJDA, C."' showing total 2 results
Start Over Author "GAJDA, C." Journal bioorganic medicinal chemistry letters
2 results on '"GAJDA, C."'

1. Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety.

Author

Vara Prasad JV, Markoski LJ, Boyer FE, Domagala JM, Ellsworth EL, Gajda C, Hagen SE, Tait BD, Lunney EA, Tummino PJ, Ferguson D, Holler T, Hupe D, Nouhan C, Gracheck SJ, VanderRoest S, Saunders J, Iyer K, and Sinz M

Subjects
Animals, Disulfides chemistry, Disulfides pharmacology, HIV drug effects, HIV Protease Inhibitors chemistry, HIV Protease Inhibitors pharmacokinetics, HIV Protease Inhibitors pharmacology, Mice, Models, Molecular, Pyrones chemistry, Pyrones pharmacology, Structure-Activity Relationship, Sulfonic Acids pharmacology, Disulfides chemical synthesis, HIV Protease Inhibitors chemical synthesis, Pyrones chemical synthesis, Sulfonic Acids chemistry
Abstract

Dihydropyran-2-ones possessing a sulfamate moiety at the 4-position of the thiophenyl ring were designed to reach S3' pocket of the HIV protease. Synthetic routes for the preparation of thiotosylates possessing 3-(2-t-butyl-5-methyl-4-sulfamate) phenylthio moiety were established. SAR of various sulfamate analogs including HIV protease binding affinities, antiviral activities and therapeutic indices will be described.

Published
1999
Full Text
View/download PDF

2. Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing achiral 3-(4-amino/carboxamide-2-t-butyl,5-methylphenyl thio) moiety: antiviral activities and pharmacokinetic properties.

Author

Vara Prasad JV, Boyer FE, Domagala JM, Ellsworth EL, Gajda C, Hagen SE, Markoski LJ, Tait BD, Lunney EA, Tummino PJ, Ferguson D, Holler T, Hupe D, Nouhan C, Gracheck SJ, VanderRoest S, Saunders J, Iyer K, Sinz M, and Brodfuehrer J

Subjects
Animals, Anti-HIV Agents pharmacology, Crystallography, X-Ray, Dogs, Inhibitory Concentration 50, Kinetics, Mice, Models, Molecular, Structure-Activity Relationship, HIV Protease Inhibitors chemical synthesis, HIV Protease Inhibitors pharmacokinetics, Pyrans chemical synthesis, Pyrans pharmacokinetics
Abstract

Dihydropyran-2-ones possessing amino and carboxamide functionalities on 3-SPh (2-tert-butyl, 5-methyl) ring were synthesized and evaluated for their antiviral activities. Both the enantiomers of inhibitor 15 were synthesized. The in vitro resistance profile, inhibitory activities against cytochrome P450 isozymes and pharmacokinetic properties of inhibitor 15S will be discussed.

Published
1999
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results