Bethegnies G, Marcincal-Lefebvre A, Brunet C, Cazin M, Damas J
Laboratoire de Chimie Organique, Faculté de Pharmacie Université de Lille, France.
Farmaco. 1989 Jul-Aug;44(7-8):683-94.
Several acid and closely related non acid derivatives of 2-phenylthio- and 4-phenylthio-N-acyl phenylamines have been synthesized and tested in vivo, on the carrageenan RFE assay, and in vitro, on prostaglandin synthesis inhibition assay. Compound (XV c), bearing a propanoic acid substituent together with a p-chlorobenzoyl group situated on nitrogen atom in the 2-position, showed a 79% edema reduction (300 mg/kg p.o.) 6 hours after carrageenan injection, but no activity in vitro. The benzyl alcohols (XIV m) and (XIV n), on the contrary, inhibited PG synthesis; their lack of activity in vivo could be interpreted as the result of their oxidation to the inactive benzoic acids (XIV g) and (XIV h).
已合成了几种2-苯硫基和4-苯硫基-N-酰基苯胺的酸及其密切相关的非酸衍生物，并在体内通过角叉菜胶足肿胀实验进行了测试，在体外通过前列腺素合成抑制实验进行了测试。化合物（XV c）在2位的氮原子上带有丙酸取代基以及对氯苯甲酰基，在注射角叉菜胶6小时后口服300 mg/kg显示出79%的水肿减轻，但在体外无活性。相反，苄醇（XIV m）和（XIV n）抑制前列腺素合成；它们在体内缺乏活性可解释为它们被氧化为无活性的苯甲酸（XIV g）和（XIV h）的结果。
