Structure-activity relationships of tetramethylpiperidine-substituted phenazines against Mycobacterium leprae in vitro.
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.
Franzblau
S G
SG
Gillis W. Long Hansen's Disease Center, Carville, Louisiana 70721.
White
K E
KE
O'Sullivan
J F
JF
D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D002991:Clofazimine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D009166:Mycobacterium leprae / Q000187:drug effects*; D010619:Phenazines / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D010619:Phenazines; D010880:Piperidines; D002991:Clofazimine