ANTIALLERGY AGENTS .1. 1,6-DIHYDRO-6-OXO-2-PHENYLPYRIMIDINE-5-CARBOXYLIC ACIDS AND ESTERS

被引：41

作者：

JUBY, PF

HUDYMA, TW

BROWN, M

ESSERY, JM

PARTYKA, RA

机构：

[1] Research Division, Bristol Laboratories, Division of Bristol-Myers Company, Syracuse

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1979年 / 22卷 / 03期

关键词：

D O I：

10.1021/jm00189a009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of some l, 6-dihydro-6-oxo-2-phenylpyrimidine-5-carboxylic acids and esters with potent oral and intravenous antiallergic activity against passive cutaneous anaphylaxis in the rat is described. Requirements for high activity include a free NH group in the pyrimidinone nucleus and a small to medium size ortho alkoxy or alkenyloxy group on the phenyl ring. It is suggested that in the case of the highly active compounds hydrogen bonding occurs between a nitrogen of the pyrimidine ring and the ethereal oxygen. The nature of this bonding and its possible contribution to an optimum configuration for the molecules is discussed. © 1979, American Chemical Society. All rights reserved.

引用

页码：263 / 269

页数：7

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