Synthesis and biological activities of novel β-carbolines as PDE5 inhibitors

被引：16

作者：

Sui, ZH ^{[1
]}

Guan, JH ^{[1
]}

Macielag, MJ ^{[1
]}

Jiang, WQ ^{[1
]}

Qiu, YH ^{[1
]}

Kraft, P ^{[1
]}

Bhattacharjee, S ^{[1
]}

John, TM ^{[1
]}

Craig, E ^{[1
]}

Haynes-Johnson, D ^{[1
]}

Clancy, J ^{[1
]}

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev LLC, Raritan, NJ 08869 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(02)01036-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of N-2-furoyl and N(2)pyrimidinyl beta-carbolines was discovered to possess potent inhibitors activity against PDE5. During the synthesis we developed a tandem resin quenching protocol. which allowed us to synthesize large number of target compounds in a rapid fashion. Representative Compounds exhibit superior selectivity to sildenafil versus other isozymes of PDEs. and demonstrated in vivo efficacy in increasing introcavernosal pressure in dogs. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：761 / 765

页数：5

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