基于氧化固醇结合蛋白的哌啶基噻唑类新农药创制研究进展  

Research progress on oxysterol binding protein based novel piperidinylthiazole pesticide development

作　　者：吴启凡 郝泽生 范志金[1] WU Qifan;HAO Zesheng;FAN Zhijin(State Key Laboratory of Elemento-Organic Chemistry,College of Chemistry,Nankai University,Tianjin 300071,China)

机构地区：[1]南开大学化学学院元素有机化学国家重点实验室

出　　处：《农药学学报》2019年第5期595-608,共14页Chinese Journal of Pesticide Science

基　　金：国家自然科学基金(31571991,31872007);天津市人才发展特殊支持计划-高层次创新创业团队项目;天津市自然科学基金重点项目(18JCZDJC33500)

摘　　要：哌啶基噻唑类化合物最初主要应用于医药领域。2008年杜邦公司研发出首个哌啶基噻唑异噁唑啉类杀菌剂氟噻唑吡乙酮(oxathiapiprolin)后,哌啶基噻唑类化合物被发现能够通过抑制一种新的作用靶标氧化固醇结合蛋白(oxysterol binding protein,简称OSBP)而影响胆固醇类化合物的代谢,从而发挥杀菌的效果。基于OSBP的哌啶基噻唑类化合物正逐渐成为新农药创制的一个重要研究方向,本文综述了近10年来哌啶基噻唑类衍生物在农药和医药领域的发展历程,以及OSBP和氟噻唑吡乙酮的研究进展,以期对该类新农药的创制提供参考。Piperidinylthiazole derivatives were originally used in the drug discovery.After the commercialization of oxathiapiprolin which was developed as the first piperidinyl thiazole isoxazoline fungicide by DuPont in 2008,piperidinylthiazole compounds were found to inhibit fungi growth by affecting the metabolism of cholesterol through inhibiting its novel target of oxysterol binding protein(OSBP).OSBP-based piperidinylthiazole derivatives were gradually becoming one of the hot research areas for novel pesticide discovery.The development of piperidinylthiazole compounds in the fields of pesticide and medicine,and the research progress of OSBP and oxathiapiprolin in the past decade were summarized in this review to provide reference for the further development of novel pesticides.

关 键 词：氧化固醇结合蛋白 哌啶基噻唑 氟噻唑吡乙酮 生物活性 作用机制 研究进展 

分 类 号：O626[理学—有机化学]