Reference

Biochemical effects of miconazole on fungi

Biochemical effects of miconazole on fungi. II. Inhibition of ergosterol biosynthesis in Candida albicans. Van den Bossche, H.; Willemsens, G.; Cools, W.; Lauwers, W. F. J.; Le Jeune, L. (Anal. Dep., Janssen Pharm., Beerse, Belg.). Chem.-Biol. Interact., 21(1), 59-78 (English) 1978. CODEN: CBINA8. ISSN: 0009-2797. DOCUMENT TYPE: Journal CA Section: 3 (Biochemical Interactions) The effects of the antifungal agent miconazole nitrate (I nitrate) [22832-87-7] on the ergosterol [57-87-4] biosynthesis in C. albicans were investigated after in vitro contact with the drug for 1, 4, 16, and 24 h. A time- and dose-(2 ′ 10-10-10-4M) dependent inhibition of acetate-14C incorporation into ergosterol was obsd. Fifty percent inhibition of the acetate incorporation into ergosterol was found after 1 h incubation in the presence of 10-9M I. Simultaneously 24-methylenedihydrolanosterol [6890-88-6], lanosterol [79-63-0], obtusifoliol [16910-32-0], 4,14-dimethylzymosterol [21080-46-6], and 14-methylfecosterol [33886-74-7] accumulated. I also intervened to a small extent in triglyceride synthesis. However, in all circumstances studied, ergosterol biosynthesis was affected at lower doses than those interfering with the acetate incorporation into triglycerides. Sixteen and 24 h of incubation in the presence of I (310-6M) also increased fatty acid synthesis. I-induced inhibition of the C-14 sterol demethylation may be at the origin of the previously obsd. permeability changes in I-treated C. albicans.

Antimicrobial compositions for the topical treatment of acne vulgaris

Antimicrobial compositions for the topical treatment of acne vulgaris. Van Bever, Willem F. M. (Janssen Pharmaceutica N. V., Belg.). U.S. US 4446145 A 1 May 1984, 7 pp. Cont.-in-part of U.S. Ser. No. 114,813, abandoned. (English). (United States of America). CODEN: USXXAM. CLASS: IC: A61K031-415. NCL: 424273000R. APPLICATION: US 81-282975 13 Jul 1981. PRIORITY: US 80-114813 24 Jan 1980. DOCUMENT TYPE: Patent CA Section: 63 (Pharmaceuticals) Nonirritating topical compns. for the treatment of acne vulgaris consist of Bz2O2 [94-36-0] and a suitable azole deriv. (I, R1 = C1-6 alkanoyl, C1-6 hydroxyalkyl, Ph, halophenyl; R2 = aryl, aryloxy, arylthio, arylalkylthio; R3 = H, C2-6 alkynyl, lower alkoxycarbonyl and Ph, Q = CH or N and n = 0 or 1). Thus, a mixt. prepd. contg. 75.0 g Tween and 8.96 L water was added to 3600.0 g Bz2O2 paste and the mixt. sieved. Miconazole nitrate [22832-87-7] (1000 g) was added and the whole was mixed until complete wetting. The suspension was homogenized to break all agglomerations. A nonaq. emulsion was prepd. contg. 5000.0 g propylene glycol and 800.0 g Na lauryl sulfate was added to a molten mixt. contg. 6000.0 g cetyl alc. and 500.0 g white wax. The aq. emulsion was then added to the nonaq. emulsion and the mixt. was homogenized for 30 min and dild. to a total vol. of 50 L.