Kappe C O
Institute of Chemistry/Organic and Bioorganic Chemistry, Karl-Franzens-University Graz, Heinrichstrasse 28, A-8010, Graz, Austria.
Eur J Med Chem. 2000 Dec;35(12):1043-52. doi: 10.1016/s0223-5234(00)01189-2.
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.
1893年，P. 比吉内利首次报道了通过芳香醛、尿素和乙酰乙酸乙酯的三组分缩合反应合成官能化的3,4-二氢嘧啶-2(1H)-酮（DHPMs）。在过去几十年中，这类比吉内利型二氢嘧啶酮因其与该杂环骨架相关的有趣药理特性而受到了相当多的关注。在本综述中，我们重点介绍了该领域的最新进展，尤其关注最近开发的作为钙通道调节剂、α(1a)肾上腺素能受体选择性拮抗剂以及靶向有丝分裂机制的化合物的DHPMs。
