Raman K, Parmar S S, Kumar S, Brumleve S J
Pharmacology. 1978;17(1):56-60. doi: 10.1159/000136835.
Ten 2-[acyl-N-(substituted benzylidene)hydrazino]5-phenyltetrazoles were synthesized, characterized and evaluated for anti-inflammatory and antiproteolytic activity. The protection afforded by these tetrazoles at a dose of 100 mg/kg i.p., against carrageenin-induced edema in rats, ranged from 11 to 46%. Oxyphenbutazone (40 mg/kg i.p.), and hydrocortisone (10 mg/kg i.p.), used as reference drugs, exhibited protection of 54 and 47%, respectively. The antiproteolytic activity of these tetrazoles, as reflected by their ability to inhibit trypsin-induced hydrolysis of bovine serum albumin, ranged from 17 to 57%. The antiproteolytic activity was found to be unrelated to the anti-inflammatory activity possessed by these tetrazoles.
合成了10种2-[酰基-N-(取代亚苄基)肼基]-5-苯基四唑,并对其进行了表征以及抗炎和抗蛋白水解活性评估。这些四唑以100mg/kg腹腔注射给药时,对大鼠角叉菜胶诱导的水肿的保护率为11%至46%。作为对照药物的羟布宗(40mg/kg腹腔注射)和氢化可的松(10mg/kg腹腔注射)的保护率分别为54%和47%。这些四唑的抗蛋白水解活性,通过其抑制胰蛋白酶诱导的牛血清白蛋白水解的能力来反映,范围为17%至57%。发现这些四唑的抗蛋白水解活性与它们所具有的抗炎活性无关。