p38 MAP kinase inhibitors.: Part 1:: Design and development of a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold

被引：43

作者：

Natarajan, SR

Wisnoski, DD

Singh, SB

Stelmach, JE

O'Neill, EA

Schwartz, CD

Thompson, CM

Fitzgerald, CE

O'Keefe, SJ

Kumar, S

Hop, CECA

Zaller, DM

Schmatz, DM

Doherty, JB

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Inflammat Res, Rahway, NJ 07065 USA

[3] Merck Res Labs, Dept Drug Metab, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(02)00876-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new class of p38 antagonists based on 3,4-dihydropyrido[3,2,-d]pyrimidine scaffold has been developed. These inhibitors exhibit unprecedented selectivity towards p38 over other very closely related kinases. Compounds 25, 33, and 34 were identified as benchmark analogues for follow-up studies. They show good potency for enzyme inhibition and excellent functional activity. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：273 / 276

页数：4

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