Quinazolines: Combined type 3 and 4 phosphodiesterase inhibitors.

被引：22

作者：

Charpiot, B ^{[1
]}

Brun, J ^{[1
]}

Donze, I ^{[1
]}

Naef, R ^{[1
]}

Stefani, M ^{[1
]}

Mueller, T ^{[1
]}

机构：

[1] Novartis Pharma AG, Res, CH-4002 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(98)00508-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of quinazolines has been prepared and evaluated for its ability to inhibit cyclic AMP phosphodiesterase type 3, type 4A, 4B and 4D. The most potent inhibitors showed IC50 values in the nanomolar range far type 3 and type 4 isoforms and bind with high affinity to the [H-3]rolipram binding site. These quinazolines represent a new family of potent mixed PDE 3 / 4 inhibitors and are expected to have a therapeutic potential. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：2891 / 2896

页数：6

共 26 条

[1]

ANDRIEVSKII AM, 1993, ZH ORG KHIM+, V29, P1828

[2] ISOLATION OF A CDNA-ENCODING A HUMAN ROLIPRAM-SENSITIVE CYCLIC-AMP PHOSPHODIESTERASE (PDE IVD) [J].