Wade P C, Vogt B R, Kissick T P, Simpkins L M, Palmer D M, Millonig R C
J Med Chem. 1982 Mar;25(3):331-3. doi: 10.1021/jm00345a021.
Certain 1-acyl-3-phenyl-5-alkyltriazoles were synthesized and evaluated for antiinflammatory activity using the mouse active Arthus (MAA) reaction as the test system. Modification of the acyl group, 4-phenyl substituent, and alkyl group led to the selection of the most active member of this series, 1-acetyl-3-(4-chlorophenyl)-5-methyl-1,2,4-triazole (3c), for further evaluation as a novel nonacidic antiinflammatory agent.
合成了某些1-酰基-3-苯基-5-烷基三唑,并以小鼠主动Arthus(MAA)反应作为测试系统评估其抗炎活性。对酰基、4-苯基取代基和烷基进行修饰后,筛选出了该系列中活性最强的成员1-乙酰基-3-(4-氯苯基)-5-甲基-1,2,4-三唑(3c),作为一种新型非酸性抗炎药进行进一步评估。