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Design, Synthesis and Fungicidal Activity of Novel 2‐aryl‐thiazole Derivatives Containing Saccharin Motif
Author(s) -
Huang Danling,
Liao Min,
Zhang Tianyuan,
You Shuyan,
Zhou YunFeng,
Cheng YongXian
Publication year - 2020
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.202003616
Subject(s) - thiazole , botrytis cinerea , sclerotinia sclerotiorum , aryl , chemistry , acetamide , stereochemistry , saccharin , proton nmr , fungicide , organic chemistry , biology , botany , alkyl , endocrinology
A series of novel 2‐aryl‐thiazole derivatives containing saccharin were designed and synthesized by a facile method, and their structures were characterized by 1 H NMR, 13 C NMR and HMRS. Biological tests indicated that the parts of 2‐aryl‐thiazole derivatives possess potent fungicidal activities against Sclerotinia sclerotiorum , Botrytis cinerea , and Alternaria altanata . Especially, N ‐((2‐(4‐chlorophenyl)thiazol‐4‐yl)methyl)‐4‐(1,1‐dioxido‐3‐oxobenzo[d]isothia‐zol‐2(3H)‐yl)butanamide ( 7 p ) displays inhibition rates of 49.2 % and 41.9 % at a concentration of 10 mg/L against S. sclerotiorum and B. cinerea respectively, while 2‐(1,1‐dioxido‐3‐oxobenzo[d]isothiazol‐2(3H)‐yl)‐ N ‐((2‐(4‐methoxyphenyl)thiazol‐4‐yl)methyl)acetamide ( 7 f) shows an inhibition rate of 53.3 % at a concentration of 10 mg/L against A. altanata . Furthermore, the structure‐activity relationship was discussed. It suggested that the 2‐aryl‐thiazole group can be considered as a precursor structure for further design of fungicides.