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Discovery of a series of aminopiperidines as novel iNOS inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Jan 01; Vol. 18 (1), pp. 336-43. Date of Electronic Publication: 2007 Oct 25. - Publication Year :
- 2008
-
Abstract
- Nitric oxide (NO), a mediator of various physiological and pathophysiological processes, is synthesized by three isozymes of nitric oxide synthase (NOS). Potential candidate clinical drugs should be devoid of inhibitory activity against endothelial NOS (eNOS), since eNOS plays an important role in maintaining normal blood pressure and flow. A new series of aminopiperidines as potent inhibitors of iNOS were identified from a HTS lead. From this study, we identified compound 33 as a potent iNOS inhibitor, with >25-fold selectivity over eNOS and 16-fold selectivity over nNOS.
- Subjects :
- Amines chemistry
Binding Sites
Drug Design
Enzyme Inhibitors chemistry
Humans
Inhibitory Concentration 50
Models, Molecular
Nitric Oxide Synthase Type I antagonists & inhibitors
Nitric Oxide Synthase Type I metabolism
Nitric Oxide Synthase Type II metabolism
Nitric Oxide Synthase Type III antagonists & inhibitors
Nitric Oxide Synthase Type III metabolism
Piperidines chemistry
Structure-Activity Relationship
Amines chemical synthesis
Amines pharmacology
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors pharmacology
Nitric Oxide Synthase Type II antagonists & inhibitors
Piperidines chemical synthesis
Piperidines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18024030
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.10.073