Structure-activity relationships of tetramethylpiperidine-substituted phenazines against Mycobacterium leprae in vitro
Author(s) -
Scott G. Franzblau,
Karen E. White,
John O’Sullivan
Publication year - 1989
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.33.11.2004
Subject(s) - mycobacterium leprae , alkoxy group , in vitro , chemistry , structure–activity relationship , biological activity , partition coefficient , stereochemistry , biochemistry , organic chemistry , biology , leprosy , alkyl , immunology
In a previous study of structure-activity relationships of selected phenazines against Mycobacterium leprae in vitro, compounds containing a 2,2,6,6-tetramethylpiperidine substitution at the imino nitrogen were most active. Therefore, the effect of substitution at the para positions of the phenyl and anilino groups in tetramethylpiperidine-substituted phenazines was assessed. As determined by radiorespirometry, activity in ascending order was observed in compounds substituted with hydrogens or fluorines, ethoxy groups, methyl groups, chlorines, and bromines and correlated with partition coefficients in octanol-water.
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