高等学校化学学报Issue(2)：281-285,5.DOI:10.7503/cjcu20130551
新型取代苯基噁唑类化合物的设计、合成及生物活性
Design, Synthesis and Biological Activity of Novel Substituted Phenyl Oxazol Based Compounds
摘要
Abstract
Several famous bioactive heterocycles such as oxazole, imidazolidine and thiazolidine are widely used in both pharmaceutical and pesticide industry. To find new lead compounds with favorable biological ac-tivities, a series of novel substituted phenyl oxazol based compounds containing 2-nitroaminoimidazoline or thiazolidine was designed via the method of linking active sub-structures. The target compounds were synthe-sized from substituted benzoic acid in three steps. Their structures were confirmed by 1 H NMR and elemental analysis. The preliminary bioassay results indicated that some target compounds showed obvious inhibitory ac-tivities against Gibberella saubinetii, Rhizoctonia solani, Botrytis cinerea and Alternaria solan. Especially, compound 5q, with 62% and 86% inhibition rate against Gibberella saubinetii and Botrytis cinerea, respective-ly, exhibited equivalent activity to Polyoxin B with 57% and 85% inhibition rate at a concentration of 100μg/mL. The structure-activity relationship indicated that the type and position of substituent on the benzene ring would influence the activity obviously. The halogen substituent was favorable to activity. Besides, com-pounds with ortho-substituent showed better activity than those with meta or para-substituent.关键词
噁唑/咪唑烷/噻唑烷/生物活性Key words
Oxazole/Imidazoline/Thiazolidine/Biological activity分类
化学化工引用本文复制引用
刘少华,凌云,李宏月,徐丹,杨新玲..新型取代苯基噁唑类化合物的设计、合成及生物活性[J].高等学校化学学报,2014,(2):281-285,5.基金项目
国家“十二五”科技支撑计划项目(批准号:2011BAE06B05-5)和国家自然科学基金(批准号:21132003)资助.@@@@Supported by the National Scientific and Technology Supporting Program of China(No.2011BAE06B05-5) and the National Natural Science Foundation of China(No.21132003) （批准号:2011BAE06B05-5）
