Efficacy of some synthesized thiazoles against dermatophytes

作者：Ouf S A^*; Abu Taleb A M; Tharwat N A; Geweely N S

来源：Journal de Mycologie Medicale, 2013, 23(4): 230-236.

DOI：10.1016/j.mycmed.2013.07.056

• Antifungal agents
• Azoles
• Dermatophytes
• Keratinase
• Ergosterol

Twelve thiazoles and their fused derivatives were tested for their antimicrobial activity against Trichophyton rubrum, T terrestre, Epidermophyton floccosum, and Microsporum gypseum. Most of the synthesized compounds were inhibitory to the tested fungi. The most effective compound was 5-(4-ethoxybenzylidene-4,5-dihydro-4-oxothiazol-2-yl)-N,3-diphenylbut-2-namide (3c) followed by 2-(4-oxo-4,5-dihydrothiazol-2-yl)-3-phenyl-but-2-enoic acid-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl)-amide (2b). These compounds were more efficacious than terbinafine, the reference drug. The tested compounds caused variable reduction in the activity of keratinase of the dermatophytes, depending on the azole derivative and the test fungus. Thiazole derivatives (2b) and (3c) exhibited the highest efficacy in decreasing ergosterol biosynthesis of the tested dermatophytes. The treatment of guinea pigs with compound (3c) induced complete curing in the case of all the test dermatophytes 30 days post-treatment. The percent curing for compounds (3c) and (2b) was better than the reference drug.

• 出版日期2013-12