ANTIBACTERIAL AND ANTIFUNGAL AGENTS .15. SYNTHESIS AND ANTIFUNGAL ACTIVITY OF STRUCTURAL ANALOGS OF BIFONAZOLE AND KETOCONAZOLE

The synthesis and antifungal activities of the cis- and trans-1-acetyl-4-{4-[[2-(1,1'-biphenyl-4-yl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl}piperazines 3 and 4 are reported. Stereochemical assignments to diastereomeric pairs of cis/trans isomers were made on the basis of H-1- and C-13-NMR data. Among test derivatives the best activity was shown by the benzoyl esters of the cis- and trans-[2-)1,1'-biphenyl-4-yl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methanols 9 and 10.