Hori M, Iemura R, Hara H, Ozaki A, Sukamoto T, Ohtaka H
Pharmaceuticals Research Center, Kanebo Ltd., Osaka, Japan.
Chem Pharm Bull (Tokyo). 1990 May;38(5):1286-91. doi: 10.1248/cpb.38.1286.
Several types of quinazoline derivatives were prepared and examined for anticonvulsive and antihypoxic activities. Many compounds showed potent anticonvulsive activity, and their anticonvulsive profile is similar to that of phenytoin. The analysis of quantitative structure-activity relationships indicated that the anticonvulsive activity was parabolically related to the lipophilicity of the compounds. Most of the 4-alkoxyquinazolines showed potent anticonvulsive and antihypoxic activities. It is confirmed that there is a good correlation between the potencies of these activities.
制备了几种喹唑啉衍生物,并对其抗惊厥和抗缺氧活性进行了研究。许多化合物显示出强效抗惊厥活性,其抗惊厥特征与苯妥英相似。定量构效关系分析表明,抗惊厥活性与化合物的亲脂性呈抛物线关系。大多数4-烷氧基喹唑啉显示出强效抗惊厥和抗缺氧活性。证实这些活性的效力之间存在良好的相关性。