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Discovery of a series of aminopiperidines as novel iNOS inhibitors.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Le Bourdonnec B,Leister LK,Ajello CA,Cassel JA,Seida PR,O'Hare H,Gu M,Chu GH,Tuthill PA,DeHaven RN,Dolle RE

doi

10.1016/j.bmcl.2007.10.073

subject

Has Abstract

pub_date

2008-01-01 00:00:00

pages

336-43

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)01254-1

journal_volume

18

pub_type

杂志文章

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