Buckler R T, Hartzler H E, Phillips B M
J Med Chem. 1975 May;18(5):509-13. doi: 10.1021/jm00239a015.
A series of 34 beta-arylamidoacrylic acids was prepared and examined for antiinflammatory activity. These compounds are vinylogous carbamic acids, and several displayed activity equal to phenylbutazone in the rat pleural effusion model. Highest activity was associated with structures bearing halogen and cyano substituents. Amides were inactive.
制备了一系列34种β-芳基氨基丙烯酸,并对其抗炎活性进行了研究。这些化合物是乙烯型氨基甲酸,其中几种在大鼠胸腔积液模型中显示出与苯基丁氮酮相当的活性。最高活性与带有卤素和氰基取代基的结构有关。酰胺没有活性。