Walsh D A, Shamblee D A, Welstead W J, Sancilio L F
J Med Chem. 1982 Apr;25(4):446-51. doi: 10.1021/jm00346a022.
Several substituted 2-aminophenylacetic acid derivatives were prepared and tested for in vitro prostaglandin synthetase inhibition activity and for in vivo antiinflammatory activity. The 2-amino substituent is beneficial to potency in the inhibition of prostaglandin synthetase for the 3-phenoxy, 4-phenyl, and 3-benzoyl series, but only the 3-benzoyl series shows increased antiinflammatory potency in the in vivo assay.
制备了几种取代的2-氨基苯乙酸衍生物，并对其进行体外前列腺素合成酶抑制活性和体内抗炎活性测试。对于3-苯氧基、4-苯基和3-苯甲酰基系列，2-氨基取代基有利于提高前列腺素合成酶抑制活性，但只有3-苯甲酰基系列在体内试验中显示出增强的抗炎效力。
