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抗炎药。4. 2-氨基-3-苯甲酰基苯乙酸和2-氨基-3-(4-氯苯甲酰基)苯乙酸潜在前药的合成与生物学评价。

Antiinflammatory agents. 4. Syntheses and biological evaluation of potential prodrugs of 2-amino-3-benzoylbenzeneacetic acid and 2-amino-3-(4-chlorobenzoyl)benzeneacetic acid.

作者信息

Walsh D A, Moran H W, Shamblee D A, Welstead W J, Nolan J C, Sancilio L F, Graff G

机构信息

Department of Chemical Research, A.H. Robins Company, Richmond, Virginia 23261-6609.

出版信息

J Med Chem. 1990 Aug;33(8):2296-304. doi: 10.1021/jm00170a039.

DOI:10.1021/jm00170a039
PMID:2115589
Abstract

A series of potential prodrugs of 2-amino-3-benzoylbenzeneacetic acid (amfenac) and 2-amino-3-(4-chlorobenzoyl)benzeneacetic acid were synthesized and evaluated for their cyclooxygenase inhibiting properties, antiinflammatory potency, and gastrointestinal irritation liability. One compound, 2-amino-3-(4-chlorobenzoyl)benzeneacetamide, possessed a therapeutic index 1 order of magnitude greater than that of indomethacin.

摘要

合成了一系列2-氨基-3-苯甲酰基苯乙酸（氨芬酸）和2-氨基-3-（4-氯苯甲酰基）苯乙酸的潜在前药，并对其环氧合酶抑制特性、抗炎效力和胃肠道刺激倾向进行了评估。一种化合物，2-氨基-3-（4-氯苯甲酰基）苯乙酰胺，其治疗指数比吲哚美辛高1个数量级。

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