Manoury P M, Dumas A P, Najer H, Branceni D, Prouteau M, Lefevre-Borg F M
J Med Chem. 1979 May;22(5):554-9. doi: 10.1021/jm00191a017.
A series of (4-substituted phenyl-1-piperazinyl)alkyl 2-aminobenzoates and 2-aminonicotinates has been prepared and screened for analgesic and antiinflammatory properties in mice and rats. The tabulated results reveal several 2-(4-substituted phenyl-1-piperazinyl)ethyl 2-(7- or 8-substituted 4-quinolinylamino)benzoates to be six to nine times more potent analgesics than the reference compounds (glafenine and aminopyrine) and to possess minor antinflammatory activity. Compound 45, 2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl 2-[[7-(trifluoromethyl)-4-quinolinyl]amino]benzoate (antrafenine), showed marked analgesic activity, long duration of action, and excellent tolerance in pharmacological and toxicological studies, as well as in clinical trials.
已制备了一系列（4-取代苯基-1-哌嗪基）烷基2-氨基苯甲酸酯和2-氨基烟酸酯，并在小鼠和大鼠中筛选了其镇痛和抗炎特性。列表结果显示，几种2-（4-取代苯基-1-哌嗪基）乙基2-（7-或8-取代4-喹啉基氨基）苯甲酸酯的镇痛效力比参考化合物（格拉非宁和氨基比林）强6至9倍，并具有轻微的抗炎活性。化合物45，2-[4-[3-（三氟甲基）苯基]-1-哌嗪基]乙基2-[[7-（三氟甲基）-4-喹啉基]氨基]苯甲酸酯（安他芬宁）在药理和毒理学研究以及临床试验中均显示出显著的镇痛活性、长效作用和优异的耐受性。
