Title of article
Discovery of a series of aminopiperidines as novel iNOS inhibitors
Author/Authors
Bertrand Le Bourdonnec، نويسنده , , Lara K. Leister، نويسنده , , Christopher A. Ajello، نويسنده , , Joel A. Cassel، نويسنده , , Pamela R. Seida، نويسنده , , Heather O’Hare، نويسنده , , Minghua Gu، نويسنده , , Guohua Chu، نويسنده , , Paul A. Tuthill، نويسنده , , Robert N. DeHaven، نويسنده , , Roland E. Dolle، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
8
From page
336
To page
343
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.
Keywords
Aminopiperidines , inhibitors , iNOS
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798974
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