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HERO ID
4280087
Reference Type
Journal Article
Title
Design, Synthesis and Biological Activity of Novel Substituted Phenyl Oxazol Based Compounds
Author(s)
Liu Shaohua; Ling Yun; Li Hongyue; Xu Dan; Yang Xinling
Year
2014
Is Peer Reviewed?
1
Journal
Gaodeng Xuexiao Huaxue Xuebao / Chemical Journal of Chinese Universities
ISSN:
0251-0790
Volume
35
Issue
2
Page Numbers
281-285
DOI
10.7503/cjcu20130551
Web of Science Id
WOS:000332918400012
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 activities, 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 synthesized from substituted benzoic acid in three steps. Their structures were confirmed by H-1 NMR and elemental analysis. The preliminary bioassay results indicated that some target compounds showed obvious inhibitory activities 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, respectively, exhibited equivalent activity to Polyoxin B with 57% and 85% inhibition rate at a concentration of 100 mu g/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, compounds with ortho-substituent showed better activity than those with meta or para-substituent.
Keywords
Oxazole; Imidazoline; Thiazolidine; Biological activity
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