Ouf S A, Taleb A M Abu, Tharwat N A, Geweely N S
Department of Biology, Faculty of Science, Taibah University, Almadinah Almunawwarah, Saudi Arabia; Botany Department, Faculty of Science, Cairo University, Giza 12613, Egypt.
J Mycol Med. 2013 Dec;23(4):230-6. doi: 10.1016/j.mycmed.2013.07.056. Epub 2013 Oct 12.
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.
测试了12种噻唑及其稠合衍生物对红色毛癣菌、土曲霉、絮状表皮癣菌和石膏样小孢子菌的抗菌活性。大多数合成化合物对测试真菌具有抑制作用。最有效的化合物是5-(4-乙氧基亚苄基-4,5-二氢-4-氧代噻唑-2-基)-N,3-二苯基丁-2-酰胺(3c)，其次是2-(4-氧代-4,5-二氢噻唑-2-基)-3-苯基-丁-2-烯酸-(3-氰基-4,5,6,7-四氢苯并[b]噻吩-2-基)-酰胺(2b)。这些化合物比参比药物特比萘芬更有效。根据唑衍生物和测试真菌的不同，测试化合物对皮肤癣菌角质酶活性的降低程度各不相同。噻唑衍生物(2b)和(3c)在降低测试皮肤癣菌麦角甾醇生物合成方面表现出最高的功效。用化合物(3c)治疗豚鼠，在治疗后30天，所有测试皮肤癣菌均完全治愈。化合物(3c)和(2b)的治愈率优于参比药物。
