Synthesis and biological evaluation of [alpha-(1,5-disubstituted 1H-pyrazol-4-yl)benzyl]azoles, analogues of bifonazole

A series of pyrazole analogues of bifonazole, an antifungal drug used in cl inical practice, 2a-h and 4a-b were synthesized and tested in vitro against Candida albicans, Cryptococcus neoformans and Aspergillus fumigatus, with no significant results. Imidazoles 2a-h were also tested in vivo for antiar rhythmic and antihypertensive activities; two of these compounds showed mod erate activity against ventricular fibrillation caused by aconitine in rats . The above compounds were prepared by reaction of phenyl[5 substituted 1-p henyl (or 1-methyl)-1H-pyrazol-4-yl]methanols with N,N'-carbonyldiimidazole (2a-h) or of the respective chloro derivatives with 1H-1,2,4-triazole (4a- h). (C) 1999 Elsevier Science S.A. All rights reserved.