Kaltenbronn J S, Scherrer R A, Short F W, Jones E M, Beatty H R, Saka M M, Winder C V, Wax J, Williamson W R
Arzneimittelforschung. 1983;33(4A):621-7.
A large series of N-arylanthranilic acids has been prepared. Many of these compounds show high anti-inflammatory activity as measured by the anti-UV-erythema test. From this series have come the clinically useful non-steroidal anti-inflammatory agents, flufenamic acid (Arlef), mefenamic acid (Ponstel), and the latest and most potent agent, N-(2,6-dichloro-m-tolyl)anthranilic acid (meclofenamic acid, Meclomen = the sodium salt). The structure-activity relationships of this series is discussed and a graphical representation is presented which allows the prediction of activity of new agents.
已制备了一大系列的N-芳基邻氨基苯甲酸。通过抗紫外线红斑试验测定，其中许多化合物显示出高抗炎活性。临床上有用的非甾体抗炎药氟芬那酸（阿乐芬）、甲芬那酸（扑湿痛）以及最新且最有效的药物N-（2,6-二氯间甲苯基）邻氨基苯甲酸（甲氯芬那酸，甲氯灭酸 = 钠盐）均来自该系列。讨论了该系列的构效关系，并给出了一个图表，可用于预测新药物的活性。
