Synthesis and pharmacological evaluation of N-substituted 4,6-diaryl-3-pyridazinones as Analgesic, antiinflammatory and antipyretic agents.
作者:Catherine RUBAT、Pascal COUDERT、Pierre TRONCHE、Jeanine BASTIDE、Pierre BASTIDE、Anne-Marie PRIVAT
DOI:10.1248/cpb.37.2832
日期:——
The synthesis and the pharmacological evaluation of 19 new 4,6-diaryl-3-pyridazinones are reported. All compounds were screened for analgesic, antiinflammatory and antipyretic activities. Introduction of an arylpiperazinomethyl moiety in the 2-position of the pyridazinone ring resulted in the most potent activities. Compounds 2a, 2b, 2h and 2i exhibited a higher analgesic activity than did aspirin
报道了19种新的4,6-二芳基-3-吡嗪酮的合成和药理学评价。筛选所有化合物的镇痛,抗炎和解热活性。在哒嗪酮环的2-位引入芳基哌嗪子甲基部分导致最有效的活性。在热板试验中,化合物2a,2b,2h和2i的镇痛活性高于阿司匹林或去甲多米诺林。