DISCOVERY OF MICROMOLAR PDE-IV INHIBITORS THAT EXHIBIT MUCH REDUCED AFFINITY FOR THE [H-3]ROLIPRAM BINDING-SITE - 3-NORSORNYLOXY-4-METHOXYPHENYLMETHYLENE OXINDOLES

被引：35

作者：

MASAMUNE, H

CHENG, JB

COOPER, K

EGGLER, JF

MARFAT, A

MARSHALL, SC

SHIRLEY, JT

TICKNER, JE

UMLAND, JP

VAZQUEZ, E

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 17期

关键词：

D O I：

10.1016/0960-894X(95)00333-O

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and the in vitro properties of a novel series of potent and selective phosphodiesterase type IV (PDE IV) inhibitors is described. Despite bearing structural similarity to rolipram, several of these compounds have much reduced affinity for the [H-3]rolipram binding site.

引用

页码：1965 / 1968

页数：4

共 22 条

[1] SELECTIVE TYPE-IV PHOSPHODIESTERASE INHIBITORS AS ANTIASTHMATIC AGENTS - THE SYNTHESES AND BIOLOGICAL-ACTIVITIES OF 3-(CYCLOPENTYLOXY)-4-METHOXYBENZAMIDES AND ANALOGS [J].