Thienopyridines: Nitric oxide synthase inhibitors with potent in vivo activity

被引：23

作者：

Beaton, H

Boughton-Smith, N

Hamley, P

Ghelani, A

Nicholls, DJ

Tinker, AC

Wallace, AV

机构：

[1] AstraZeneca R&D Charnwood, Dept Med Chem, Loughborough LE11 5RH, Leics, England

[2] AstraZeneca R&D Charnwood, Dept Biosci, Loughborough LE11 5RH, Leics, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(01)00120-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5-Substituted 7-amino-4,5-tetrahydrothieno[2,3-c]pyridines and 6-substituted 4-amino-6.7-dihydrothieno[3.2-c]pyridines were shown to be exceptionally potent inhibitors of inducible and neuronal nitric oxide synthase. Selectivity and potency could be modulated by variation of the 5- or 6-substituent, Compound 3e showed potent in vivo inhibition of iNOS. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：1027 / 1030

页数：4

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