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[Antimycobacterial indole derivatives].

作者信息

Mahboobi S, Grothus G, Meindl W

机构信息

Institut für Pharmazie, Universität Regensburg.

出版信息

Arch Pharm (Weinheim). 1994 Feb;327(2):105-14. doi: 10.1002/ardp.19943270209.

Abstract

1,3-Dinitro-2-(indol-3'-yl)-propanes 3 are synthesized by Michael reaction of nitromethane with the indolylnitroethenes 2. Reaction of the aldehydes 4 and 10 with the benzylamines 12 as well as the reaction of the indolylalkylamines 6a and 9a with the benzaldehydes 11 lead to Schiff bases which are reduced to N-benzyl-(indol-3-ylmethyl)-amines 13 and N-benzyl-(indol-3-ylethyl)-amines 14, respectively; tert amines 16 are synthesized via the formamides 15, amines 18 are prepared according to Mannich. Inhibitory effects on Mycobacterium tuberculosis H 37 Ra are investigated, a structure-activity relationship is discussed.

摘要

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