Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha(1a)-adrenergic receptor antagonists

Authors
Lagu, B Tian, D Chiu, G Nagarathnam, D Fang, J Shen, QR Forray, C Ransom, RW Chang, RSL Vyas, KP Zhang, KY Gluchowski, C
Citation
B. Lagu et al., Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha(1a)-adrenergic receptor antagonists, BIOORG MED, 10(2), 2000, pp. 175-178
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
2
Year of publication
2000
Pages
175 - 178
Database
ISI
SICI code
0960-894X(20000117)10:2<175:SAEOFA>2.0.ZU;2-2
Abstract
Furo[3,4-d]pyrimidinones were found to be metabolites of dihydropyrimidinon es such as 1a-b that are subtype-selective antagonists of the alpha(1a)-adr energic 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 Elsevi er Science Ltd. All rights reserved.