Eguchi Y, Sasaki F, Sugimoto A, Ebisawa H, Ishikawa M
Institute for Medical and Dental Engineering, Tokyo Medical and Dental University, Japan.
Chem Pharm Bull (Tokyo). 1991 Jul;39(7):1753-9. doi: 10.1248/cpb.39.1753.
3-(2-Chlorophenyl)-6-ethoxycarbonyl-5,7-dimethyl-2,4(1H,3H)-quinazoline dione was newly prepared. 1-Hydrogen atoms of the compound were variously substituted in order to test for their hypotensive activities on relaxing effects of the blood vessels. The compounds with 2-(1-pyrrolidinyl) ethyl, 2-(1-piperidinyl)ethyl, 3-(dimethylamino)propyl, and 3-(N-benzyl-N-methylamino)propyl moieties showed significant activity. The 2-(1-piperidinyl)ethyl compound possessed activity approximately 23 times more potent than papaverine, however, it was less potent than cinnarizine.
新制备了3-(2-氯苯基)-6-乙氧羰基-5,7-二甲基-2,4(1H,3H)-喹唑啉二酮。为了测试该化合物1位氢原子的不同取代对血管舒张作用的降压活性，进行了相关研究。含有2-(1-吡咯烷基)乙基、2-(1-哌啶基)乙基、3-(二甲氨基)丙基和3-(N-苄基-N-甲基氨基)丙基部分的化合物显示出显著活性。2-(1-哌啶基)乙基化合物的活性约比罂粟碱强23倍，然而，它比桂利嗪的活性弱。
