Structure-activity correlations among rifamycin B amides and hydrazides.
Structure-antibacterial activity correlation equations have been developed for aseries of 44 amides and 25 hydrazides of rifamycin B in five bacterial systems. The best amide equations show that activity is a parabolic function of log P. A wide variation in log Po was found for the various bacterial systems. The most important correlation parameter in the hydrazide equations is omicron*. The significance of this finding is somewhat obscured by the high degree of collinearity among the parameters evaluated (omicron*, E-s, log P). Two rifamycin B amides were prepared and evaluated as a result of this study. The correlation equations quantitatively predicted their activity in five of six tests.
D000577:Amides / Q000494:pharmacology; D001412:Bacillus subtilis / Q000187:drug effects; D003201:Computers; D013293:Enterococcus faecalis / Q000187:drug effects; D006834:Hydrazines / Q000494:pharmacology; D007700:Kinetics; D008837:Micrococcus / Q000187:drug effects; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D012044:Regression Analysis; D012294:Rifamycins / Q000494:pharmacology; D013291:Streptococcus / Q000187:drug effects; D013329:Structure-Activity Relationship
D000577:Amides; D006834:Hydrazines; D012294:Rifamycins