Design, synthesis, and fungicidal activity evaluation of 2-methyl-5-phenylthiazole-4-carboxamides bearing morpholine, thiomorpholine, or thiomorpholine 1,1-dioxide moiety

被引：0
|
作者：
Wei, Jimin [1 ]
Chen, Lili [1 ]
Zhu, Kunfang [1 ]
Cheng, Yong-Xian [1 ]
Huang, Danling [1 ]
机构：
[1] Shenzhen Univ, Sch Pharm, Med Sch, 3688 Nanhai Rd, Shenzhen 518055, Peoples R China
来源：
CHEMISTRY OF HETEROCYCLIC COMPOUNDS | 2024年 / 60卷 / 9-10期
关键词：
morpholine derivatives; thiazole derivatives; thiomorpholine derivatives; fungicidal activity; structural optimization; structure-activity relationship; PHYTOPHTHORA; DERIVATIVES;
D O I：
10.1007/s10593-024-03372-6
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A series of 2-methyl-5-phenylthiazole derivatives were designed, synthesized, and characterized by 1H, 13C NMR spectra and HRMS. Subsequently, their antifungal activity was evaluated, and the bioassay results showed that almost all title compounds possess potential fungicidal activity against B. cinerea. [5-(4-Chlorophenyl)-2-methylthiazol-4-yl](morpholin-4-yl)methanone and {2-methyl-5-[4-(tri-fluoromethyl)phenyl]thiazol-4-yl}(thiomorpholin-4-yl)methanone displayed EC50 values of 19.6 mg/l and 15.6 mg/l respectively, against B. cinerea, showing higher potency than that of hymexazol.
引用
收藏
页码：536 / 543
页数：8
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