title: Efficacy of some synthesized thiazoles against dermatophytes.
abstract: 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 30days post-treatment. The percent curing for compounds (3c) and (2b) was better than the reference drug.
authors.affiliation: Department of Biology, Faculty of Science, Taibah University, Almadinah Almunawwarah, Saudi Arabia; Botany Department, Faculty of Science, Cairo University, Giza 12613, Egypt. Electronic address: saoufeg@yahoo.com.
authors.forename: S A
authors.initials: SA
authors.lastname: Ouf
authors.forename: A M Abu
authors.initials: AM
authors.lastname: Taleb
authors.forename: N A
authors.initials: NA
authors.lastname: Tharwat
authors.forename: N S
authors.initials: NS
authors.lastname: Geweely
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D004353:Drug Evaluation, Preclinical; D004821:Epidermophyton / Q000187:drug effects* / Q000378:metabolism; D004875:Ergosterol / Q000096:biosynthesis; D005656:Fungal Proteins / Q000032:analysis; D006168:Guinea Pigs; D008826:Microbial Sensitivity Tests; D008864:Microsporum / Q000187:drug effects* / Q000378:metabolism; D015394:Molecular Structure; D010447:Peptide Hydrolases / Q000032:analysis; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D014005:Tinea / Q000188:drug therapy* / Q000382:microbiology; D014249:Trichophyton / Q000187:drug effects* / Q000378:metabolism
chemical_list: D000935:Antifungal Agents; D005656:Fungal Proteins; D013844:Thiazoles; D010447:Peptide Hydrolases; C035855:keratinase; D004875:Ergosterol
keywords: Agents antifongiques; Antifungal agents; Azoles; Azolés; Dermatophytes; Ergosterol; Ergostérol; Keratinase; Kératinase