Structure-activity relationships of selected phenazines against Mycobacterium leprae in vitro.
Structure-activity relationships of phenazines against Mycobacterium leprae were investigated by using an in vitro radiorespirometric assay. In general, activity in ascending order was observed in compounds containing no chlorine atoms, a monochlorinated phenazine nucleus, and chlorines in the para positions of both the anilino and phenyl rings. The most active compounds contained a 2,2,6,6-tetramethylpiperidine substitution at the imino nitrogen. Most of these chlorinated phenazines were considerably more active in vitro than clofazimine (B663).
Franzblau
S G
SG
Gillis W. Long Hansen's Disease Center, Carville, Louisiana 70721.
O'Sullivan
J F
JF
D002991:Clofazimine / Q000494:pharmacology; D007917:Leprostatic Agents; D008826:Microbial Sensitivity Tests; D009166:Mycobacterium leprae / Q000187:drug effects*; D010619:Phenazines / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D007917:Leprostatic Agents; D010619:Phenazines; D002991:Clofazimine