Meindl W
Institut für Pharmazie, Universität Regensburg, Deutschland.
Arch Pharm (Weinheim). 1993 May;326(5):277-86. doi: 10.1002/ardp.19933260506.
Synthesis and testing for antimycobacterial properties (M. tuberculosis H 37 Ra, Middlebrook-7H9-broth) of 1-phenyl-1-alkylaminoalkanes, which differ from antimycobacterial N-alkylbenzylamines by an additional alkyl chain in alpha-position, is described. By variation of both alkyl chains and introduction of one or two Cl-substituents in the aromatic ring the activity increases up to an optimum within the homologous series. Overstepping optimal lipophilicity or ramification of the alkyl chains decrease activity.
本文描述了1-苯基-1-烷基氨基烷烃的合成及其抗分枝杆菌特性(结核分枝杆菌H 37 Ra,Middlebrook - 7H9肉汤培养基)的测试。1-苯基-1-烷基氨基烷烃与抗分枝杆菌的N-烷基苄胺的区别在于α位有一条额外的烷基链。通过改变两条烷基链以及在芳环中引入一个或两个氯取代基,在同系物系列中活性增加直至达到最佳值。超过最佳亲脂性或烷基链的分支会降低活性。