A QSAR STUDY OF THE BIOLOGICAL-ACTIVITIES OF SOME BENZIMIDAZOLES AND IMIDAZOPYRIDINES AGAINST BACILLUS-SUBTILIS

A set of benzimidazole (I) and imidazopyridine (II) derivatives that h ave previously been tested for their antibacterial activities against Bacillus subtilis were analyzed using the quantitative structure-activ ity relationship (QSAR) method. The activity contributions for structu ral and substituent effects were determined from the correlation equat ions, which were derived using all possible combination and stepwise r egression techniques. The best equation was chosen among the other equ ations by considering the various statistical criteria. The resulting QSAR revealed that the activity contributions of benzimidazoles and im idazopyridines against B subtilis depend almost entirely on their rela tive lipophilic character as defined by their octanol/water partition coefficients, log P. The ideal lipophilic character for the investigat ed imidazole nuclei has been found to be about 4.9.