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取代四唑基甲酰胺的抗炎和抗蛋白水解特性。

Antiinflammatory and antiproteolytic properties of substituted tetrazolycarbamides.

作者信息

Jaiswal R K, Parmar S S, Jaiswal N, James E C

出版信息

Res Commun Chem Pathol Pharmacol. 1982 Apr;36(1):161-4.

PMID:7079583
Abstract

Eight 1-(5-aryl-2-acetyltetrazolyl)-3-substituted carbamides were evaluated for their antiinflammatory and antiproteolytic properties. The protection afforded by these compounds (100 mg/Kg, i.p.) against carrageenin-induced edema in rats ranged from 10-45%. Oxyphenbutazone (40 mg/kg, i.p.) and hydrocortisone (10 mg/kg, i.p.), used as reference drugs, possessed 53% and 45% antiinflammatory activity, respectively. All substituted tetrazolyl carbamides (1 mM) possessed antiproteolytic activity which was reflected by their ability to inhibit the activity of trypsin during hydrolysis of bovine serum albumin. The degree of protection observed against trypsin-induced hydrolysis ranged from 25-62% while such an inhibition with sodium salicylate (1 mM) was 52%.

摘要

评估了8种1-(5-芳基-2-乙酰基四唑基)-3-取代脲的抗炎和抗蛋白水解特性。这些化合物(100毫克/千克,腹腔注射)对大鼠角叉菜胶诱导的水肿的保护率在10%-45%之间。作为参考药物的羟苯丁酮(40毫克/千克,腹腔注射)和氢化可的松(10毫克/千克,腹腔注射)的抗炎活性分别为53%和45%。所有取代的四唑基脲(1毫摩尔)都具有抗蛋白水解活性,这通过它们在牛血清白蛋白水解过程中抑制胰蛋白酶活性的能力得以体现。观察到的对胰蛋白酶诱导水解的保护程度在25%-62%之间,而水杨酸钠(1毫摩尔)的这种抑制率为52%。

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