SYNTHESIS AND SAR OF PHENYLAZOLES, ACTIVE AGAINST STAPHYLOCOCCUS AUREUS NEWMAN

Abstract

Series of new potent inhibitors of growth of Staphylococcus aureus Newman, based on 3,4-diphenylpyrazole and 4,5-diphenylisoxazole derivatives were discovered. Structures of interest were selectively modified to check their structure–activity relationship. Studies revealed the most essential groups in the molecule for the antimicrobial activity retention. Active compounds with good MIC range should contain both nonpolar aromatic residues and hydrogen bond donating groups. The best MIC results in selected cases were lower than 1 μg/ml.