Biarylcarboxamide inhibitors of phosphodiesterase IV and tumor necrosis factor-alpha

被引：13

作者：

Chambers, RJ

Marfat, A

Cheng, JB

Cohan, VL

Damon, DB

Duplantier, AJ

Hibbs, TA

Jenkinson, TH

Johnson, KL

Kraus, KG

Pettipher, ER

Salter, ED

Shirley, JT

Umland, JP

机构：

[1] Pfizer Central Research, Pfizer Inc., Groton

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(97)00097-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Tumor necrosis factor-alpha (TNF-alpha) has been implicated as a key mediator in the progression of rheumatoid arthritis. Inhibitors of phosphodiesterase IV (PDE IV) have been shown to inhibit the production of TNF-alpha by elevating intracellular levels of cyclic adenosine monophosphate (cAMP). Our efforts in a series of biarylcarboxamides have led to the identification of 8j (CP-353,164) as a potent inhibitor of PDE IV and TNF-alpha production. (C) 1997 Elsevier Science Ltd.

引用

页码：739 / 744

页数：6

共 14 条

[1]

BARNETTE MS, 1994, AM J RESP CRIT CARE, V149, pA209

[2]

Cohan VL, 1996, J PHARMACOL EXP THER, V278, P1356

[3] Biarylcarboxylic acids and -amides: Inhibition of phosphodiesterase type IV versus [H-3]rolipram binding activity and their relationship to emetic behavior in the ferret [J].