Gadad A K, Kittur B S, Kapsi S G, Mahajanshetti C S, Rajur S B
Department of Medicinal Chemistry, College of Pharmacy, J. N. Medical College, Belgaum, India.
Arzneimittelforschung. 1996 Nov;46(11):1082-5.
A series of 1-acyl/aracyl-3, 4-disubstituted-5-aminopyrazoles (IV) were synthesized by the reaction of 1-acyl/aracylhydrazines (I) with an appropriately substituted ketenedithioacetal (II/III). Compounds IV were tested for their analgesic activity by rat caudal immersion test and anti-inflammatory activity by carrageenin induced edema in rat paw test. 1-Benzoyl-3-mercapto-4-carboxamido-5-aminopyrazole (IVk) proved to be the most active compound of the series in both tests.
通过1-酰基/芳酰肼（I）与适当取代的烯酮二硫代缩醛（II/III）反应，合成了一系列1-酰基/芳酰基-3,4-二取代-5-氨基吡唑（IV）。通过大鼠尾部浸入试验测试化合物IV的镇痛活性，并通过角叉菜胶诱导的大鼠足爪水肿试验测试其抗炎活性。在这两种试验中，1-苯甲酰基-3-巯基-4-羧酰胺基-5-氨基吡唑（IVk）被证明是该系列中活性最高的化合物。
