Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective α1a-adrenergic receptor antagonists

被引：52

作者：

Lagu, B

Tian, D

Chiu, G

Nagarathnam, D

Fang, J

Shen, QR

Forray, C

Ransom, RW

Chang, RSL

Vyas, KP

Zhang, KY

Gluchowski, C

机构：

[1] Synapt Pharmaceut Corp, Dept Chem, Paramus, NJ 07652 USA

[2] Synapt Pharmaceut Corp, Dept Pharmacol, Paramus, NJ 07652 USA

[3] Merck Sharp & Dohme Ltd, Dept Pharmacol, W Point, PA 19486 USA

[4] Merck Sharp & Dohme Ltd, Dept Drug Metab, W Point, PA 19486 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(99)00653-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Furo[3,4-d]pyrimidinones were found to be metabolites of dihydropyrimidinones such as 1a-b that are subtype-selective antagonists of the alpha(1a)-adrenergic receptor. A versatile synthesis that provides access to furo[3,4-d]pyrimidinones in high yield and in enantiomerically pure forms is described along with structure-activity relationships in the series. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：175 / 178

页数：4

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