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

被引:1477
作者
Kappe, CO [1 ]
机构
[1] Karl Franzens Univ Graz, Inst Chem Organ & Bioorgan Chem, A-8010 Graz, Austria
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
收藏
页码:1043 / 1052
页数:10
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