Saraç S, Yarim M, Ertan M, Boydağ S, Erol K
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.
Pharmazie. 1998 Feb;53(2):91-4.
A series of 4-aryl-1,2,3,4,5,6,7,8-octahydroquinazoline-2,5-diones were synthesized by condensing urea with 1,3-cyclohexanedione and appropriate aromatic aldehydes according to the Biginelli reaction. The structures of the compounds were confirmed by elementary and spectroscopic analysis. The compounds synthesized were tested in vitro for their calcium antagonistic activities. BaCl2-induced contractions of rat ileum were inhibited dose-dependently. Compounds 3-8 exerted weak calcium antagonistic activity on smooth muscles compared with the standard nicardipine.
根据Biginelli反应，通过尿素与1,3 - 环己二酮和适当的芳香醛缩合，合成了一系列4 - 芳基 - 1,2,3,4,5,6,7,8 - 八氢喹唑啉 - 2,5 - 二酮。通过元素分析和光谱分析确定了化合物的结构。对合成的化合物进行了体外钙拮抗活性测试。BaCl₂诱导的大鼠回肠收缩呈剂量依赖性抑制。与标准硝苯地平相比，化合物3 - 8对平滑肌表现出较弱的钙拮抗活性。
