非甾体抗炎药。第17部分：立体异构的邻、间甲苯基和茴香基联苯基羟基丙酸。
Nonsteroidal anti-inflammatory agents. Part 17: Stereomeric o-, m-tolyl- and anisyl-biphenylyl-hydroxypropionic acids.
作者信息
Varoli L, Guarnieri A, Burnelli S, Ghedini N, Scapini G, Ferri S, Cavicchini E
机构信息
Dipartimento di Scienze Farmaceutiche, Facoltà di Farmacia dell'Università die Bologna, Italy.
出版信息
Pharmazie. 1988 Aug;43(8):524-6.
As a part of wider research project on chiral anti-inflammatory arylacanoic acids, the 3-(o- and m-)-(methyl and methoxy)-phenyl-2-biphenylyl-3-hydroxypropionic acids 3a-d were synthesized and resolved in their optically active erythro and threo stereomers, which were submitted to the carrageenan induced rat paw edema test. With respect to the p-isomers, only the threo p-methoxy substitution enhances the anti-inflammatory activity. Some conclusions on structure-activity relationship are discussed.
作为关于手性抗炎芳基烷酸的更广泛研究项目的一部分，合成了3-(邻位和间位)-(甲基和甲氧基)-苯基-2-联苯基-3-羟基丙酸3a-d，并将其拆分为旋光活性的赤藓型和苏阿糖型立体异构体，对这些异构体进行了角叉菜胶诱导的大鼠足爪水肿试验。关于对映异构体，只有苏阿糖型对甲氧基取代增强了抗炎活性。讨论了一些构效关系的结论。
Zotero 插件