Synthesis and quantitative structure-activity relationships of some antibacterial 3-formylrifamycin SV N-(4-substituted phenyl)piperazinoacethydrazones

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Abstract
A series of 14 3-formylrifamycin SV N-(4-substituted phenyl)piperazinoacethydrazones was synthesized and evaluated for their antimicrobial activity. The compounds were active against Bacillus subtilis, Staphylococcus aureus, Mycobacterium phlei and M. tuberculosis but not as active as rifampin. The compounds also exhibited significant activity against Clostridium perfringens and in this bacterial system some were more active than rifampin. The activity against B. subtilis depended only on lipophilicity and the regression equation was linear. A parabolic relationship between the antibacterial activity and lipophilicity of the compounds was found in S. aureus. Additionally, the activity was dependent upon the electronic and steric effects of the phenyl substituents. The sensitivity of M. phlei to the compounds correlated well with a linear combination of hydrophobic, electronic and steric parameters. No statistically significant correlation was possible between the physicochemical parameters studied and the activity of the compounds against C. perfringens and M. tuberculosis.

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