The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I

被引：20

作者：

Hulme, C

Moriarty, K

Miller, B

Mathew, R

Ramanjulu, M

Cox, P

Souness, J

Page, KM

Uhl, J

Travis, J

Huang, FC

Labaudiniere, R

Djuric, SW

机构：

[1] Rhone Poulenc Rorer Cent Res, Collegeville, PA 19426 USA

[2] Rhone Poulenc Rorer Cent Res, Dagenham, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(98)00324-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This communication describes the synthesis and in vitro evaluation of a novel potent series of phosphodiesterase type (IV) (PDE4) inhibitors. The compounds described contain an indole moiety which replaces the 'rolipram-like' 3-methoxy-4-cyclopentoxy motif. Several of the compounds presented possess low nanomolar IC50's for PDEIV inhibition. In vivo activities determined from measurement of serum TNF-alpha levels in LPS challenged mice (mouse endotoxemia model) are also reported. (C) 1998 Elsevier Science Ltd. All rights reserved.

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页码：1867 / 1872

页数：6

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