Becliconazole

Substituted 1-[(benzofuran-2-yl)-phenylmethyl]-imidazoles are a new class of potent aromatase inhibitor with in vitro IC50 values < 10 nM for certain members using human placental enzyme. At a dose of 2 mg/kg in PMSG-stimulated rats, selected compounds effectively reduce the oestradiol levels by 82-98%.

A number of experiments was performed in order to analyze the in vitro activity of two new benzofuran-imidazoles, IM/B/4-62 and IM/B/4-66. Studies included the determination of minimum inhibitory concentrations (MICs) on three culture media, at different pH values and at different inoculum sizes. Furthermore, the killing activity and induced resistance were determined. In all the experiments econazole, clotrimazole and bifonazole were the reference compounds. The best MIC values of the two new imidazoles were observed on modified Sabouraud's medium, at neutral pH and an inoculum size of 10(4) cells/ml. The two substances showed killing activity and no resistance was observed. On the whole, the more favorable results were obtained with the compound IM/B/4-66.