Tandon M, Kumar P, Bhalla T N, Tandon P, Gupta T K, Barthwal J P
Pharmacol Res Commun. 1983 Mar;15(3):253-65. doi: 10.1016/s0031-6989(83)80011-3.
Eighteen novel acetyl salicyloyl/butyroyl mercapto 1,3,4-thiadiazoles have been synthesized and characterized by their elemental analyses, IR and PMR spectral studies. Their efficacy against carrageenin induced paw oedema was tested in albino rats of either sex at a dose of 100 mg/kg p.o. In vitro antiproteolytic activity of the compounds was assessed by determining their ability to inhibit trypsin induced hydrolysis of bovine serum albumin. Active anti-inflammatory compounds were tested for their analgesic activity against aconitine induced writhing in albino mice. Approximate LD50 values were also determined in albino mice.
已合成了18种新型乙酰水杨酰基/丁酰基巯基-1,3,4-噻二唑，并通过元素分析、红外光谱和核磁共振光谱研究对其进行了表征。在雄性和雌性白化大鼠中，以100mg/kg口服剂量测试了它们对角叉菜胶诱导的爪肿胀的疗效。通过测定化合物抑制胰蛋白酶诱导的牛血清白蛋白水解的能力，评估了这些化合物的体外抗蛋白水解活性。对活性抗炎化合物进行了测试，以评估其对白化小鼠乌头碱诱导的扭体反应的镇痛活性。还测定了白化小鼠的近似半数致死量（LD50）值。
