Pyrroles and other heterocycles as inhibitors of p38 kinase

被引：110

作者：

de Laszlo, SE ^{[1
]}

Visco, D

Agarwal, L

Chang, L

Chin, J

Croft, G

Forsyth, A

Fletcher, D

Frantz, B

Hacker, C

Hanlon, W

Harper, C

Kostura, M

Li, B

Luell, S

MacCoss, M

Mantlo, N

O'Neill, EA

Orevillo, C

Pang, M

Parsons, J

Rolando, A

Sahly, Y

Sidler, K

Widmer, WR

O'Keefe, SJ

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 Pharmacol, Rahway, NJ 07065 USA

[4] Merck Res Labs, Dept Drug Metab, W Point, PA 19486 USA

[5] Purdue Univ, Dept Vet Clin Sci, W Lafayette, IN 47907 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(98)00495-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Investigation of furans, pyrroles and pyrazolones identified 3-pyridyl-2,5-diaryl-pyrroles as potent, orally bioavailable inhibitors of p38 kinase. 3-(4-pyridyl-2-(4-fluoro-phenyl)-5-(4-methylsulfinylphenyl)-pyrrole (L-167307) reduces secondary paw swelling in the rat adjuvant arthritis model: ID50 = 7.4 mg/kg/b.i.d. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：2689 / 2694

页数：6

共 22 条

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