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.