Design, Synthesis, Antifungal Activities and SARs of （R）-2-Aryl-4,5-dihydrothiazole-4-carboxylic Acid Derivatives
Design, Synthesis, Antifungal Activities and SARs of （R）-2-Aryl-4,5-dihydrothiazole-4-carboxylic Acid Derivatives作者机构：State Key Laboratory of Elemento-Organic Chemistry Collaborative Innovation Center of Chemical Science DQG Engineering ( Tianjin) Nankai University Tianjin 300071 China
出 版 物：《Chinese Journal of Chemistry》 (中国化学（英文版）)
年 卷 期：2015年第33卷第11期
页 面：1269-1275页
核心收录：
学科分类：1007[医学-药学(可授医学、理学学位)] 081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070305[理学-高分子化学与物理] 080501[工学-材料物理与化学] 0805[工学-材料科学与工程（可授工学、理学学位）] 0703[理学-化学] 10[医学]
主 题：(R)-2-aryl-4,5-dihydrothiazole-4-carboxylic acid synthesis antifungal activity structure-activity relationship
摘 要：Based on the structure of natural product 2-aryl-4,5-dihydrothiazole-4-carboxylic acid, a series of novel （R）-2-aryl-4,5-dihydrothiazole-4-carboxylic acid derivatives were designed and synthesized. Their structures were characterized by ^1H NMR, ^13C NMR and HRMS. The single crystal structure of compound 9b was determined by X-ray diffraction analysis. The antifungal activities were evaluated for the first time. The bioassay results indicated that most compounds exhibited moderate to good antifungal activities. The antifungal activities of compound 13a （against Cercospora arachidicola Hori）, 13d （against Alternaria solani）, and 16e （against Cercospora arachidieola Hori） were 61.9%, 67.3% and 61.9%, respectively, which are higher than those of the commercial fungicides chlorothalonil and carbendazim. Moreover, compound 13d exhibited excellent antifungal activities against 7 kinds of the fungi tested （66.7%, 77.3%, 63.0%, 87.9%, 70.0%, 70.0% and 80.0% at 50 μg/mL）. Therefore, 13d can be used as a new lead structure for the development of antifungal agents.
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