2. Academic Validation
  3. Discovery of a series of aminopiperidines as novel iNOS inhibitors

Discovery of a series of aminopiperidines as novel iNOS inhibitors

  • Bioorg Med Chem Lett. 2008 Jan 1;18(1):336-43. doi: 10.1016/j.bmcl.2007.10.073.
Bertrand Le Bourdonnec 1,  Lara K Leister,  Christopher A Ajello,  Joel A Cassel,  Pamela R Seida,  Heather O'Hare,  Minghua Gu,  Guo-Hua Chu,  Paul A Tuthill,  Robert N DeHaven,  Roland E Dolle
Affiliations

Affiliation

  • 1 Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA. blebourdonnec@adolor.com
PMID: 18024030 DOI: 10.1016/j.bmcl.2007.10.073
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.

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