Synthesis and preliminary pharmacological investigation of some 2-[4-(dialkylaminoalkoxy) phenyl] benzotriazoles and their N-oxides
作者:Anna Sparatore、Fabio Sparatore
DOI:10.1016/s0014-827x(97)00015-3
日期:1998.2
A set of 2-[4-(dialkylaminoalkoxy)phenyl]benzotriazoles and corresponding N-oxides was prepared. In a preliminary pharmacological investigation concerning some of these compounds, several in vitro and in vivo activities were shown. At concentrations in the range of 3-10 microM all tested compounds strongly inhibited (50-100%) the guinea pig ileum contractions induced either electrically or by means
制备了一组2- [4-(二烷基氨基烷氧基)苯基]苯并三唑和相应的N-氧化物。在有关其中一些化合物的初步药理研究中,显示了几种体外和体内活性。在3-10 microM的浓度范围内,所有测试的化合物均能强烈抑制(50-100%)电或通过多种激动剂诱导的豚鼠回肠收缩。特别令人感兴趣的是对白三烯D4的拮抗作用。化合物5b抑制了血栓烷A2,PAF和ADF(但不是花生四烯酸)诱导的血小板凝集,并增加了小鼠的出血时间。化合物5b和6b保护小鼠免受氰化钾缺氧并发挥抗高胆固醇的作用;第一种化合物产生的HPL与总血清胆固醇浓度之比低于0.92,