Biologically active dihydropyrimidones of the Biginelli-type - a literature survey

被引：1472

作者：

Kappe, CO ^{[1
]}

机构：

[1] Karl Franzens Univ Graz, Inst Chem Organ & Bioorgan Chem, A-8010 Graz, Austria

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2000年 / 35卷 / 12期

基金：

奥地利科学基金会;

关键词：

dihydropyrimidones; dihydropyridines; cardiovascular disease; calcium channel modulators; benign prostatic hyperplasia; mitotic machinery;

D O I：

10.1016/S0223-5234(00)01189-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In 1893, the synthesis of functionalized 3,4-dihydropyrimidin-2(1H)-ones (DHPMs) via three-component condensation reaction of an aromatic aldehyde, urea and ethyl acetoacetate was reported for the first time by P. Biginelli. In the past decades, such Biginelli-type dihydropyrimidones have received a considerable amount of attention due to the interesting pharmacological properties associated with this heterocyclic scaffold. In this review, we highlight recent developments in this area, with a focus on the DHPMs recently developed as calcium channel modulators, alpha (1a) adrenoceptor-selective antagonists and compounds that target the mitotic machinery. (C) 2000 Editions scientifiques et medicales Elsevier SAS.

引用

页码：1043 / 1052

页数：10