Studies on cardiotonic agents. III. Synthesis of 1-(1-(6,7-dimethoxy-4-quinazolinyl)-4-piperidinyl)-3-substituted 2-imidazolidinone and 2-imidazolidinethione derivatives.
作者:Yuji NOMOTO、Hiroyuki OBASE、Haruki TAKAI、Tadashi HIRATA、Masayuki TERANISHI、Joji NAKAMURA、Tetsuji OHNO、Kazuhiro KUBO
DOI:10.1248/cpb.38.2467
日期:——
A series of 1-[1-(6,7-dimethoxy-4-quinazolinyl)-4-piperidinyl]-3-substituted 2-imidazolidinone and 2-imidazolidinethione derivatives was synthesized and examined for cardiotonic activity in anesthetized dogs. Alkylation of the 2-imidazolidinone (1) afforded the N-alkylated products, while alkylation of the 2-imidazolidinethione (12) afforded the S-alkylated derivatives accompanied with a small quantity
合成了一系列的[[1-(1-,6,7-二甲氧基-4-喹唑啉基)-4-哌啶基] -3-取代的2-咪唑啉酮和2-咪唑烷硫酮衍生物,并检查了麻醉狗的强心活性。2-咪唑啉酮(1)的烷基化得到N-烷基化的产物,而2-咪唑烷硫酮(12)的烷基化得到S-烷基化的衍生物以及少量的N-烷基化的产物。N-烷基化的衍生物通常显示出有效的活性,而S-烷基化的衍生物则显示出较弱的活性。在哌啶和咪唑烷酮部分之间插入烷基通常会导致活性下降。