Design, Synthesis and Fungicidal Activity of Novel 2‐aryl‐thiazole Derivatives Containing Saccharin Motif

Abstract

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-(4methoxyphenyl)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.

Synthesis and Fungicidal Activities of Benzofuran‐Substitutes Cinnamamide Compounds

“…Oomycetes are one of the important pathogens that cause many crop diseases [1–3] . Oomycetes have a wide variety that are harmful after infection.…”

“…Oomycetes are one of the important pathogens that cause many crop diseases. [1][2][3] Oomycetes have a wide variety that are harmful after infection. They spread rapidly among different crops and have extremely bad effects on many crops and floral plants, resulting in losses of nearly one billion all over the world and seriously threatening world food security and ecosystem security.…”

Structural Modification of Saccharin Containing 2‐Aminothiazole As Potential Fungicidal Agents

“…In our previous works, [22] to dig out chemisty-diverse thiazole derivatives with fungicidal activity, we have designed and synthesized a series of compounds via molecular hybridization strategy, combining diimide-like saccharin with thiazole skeleton. However, their bioactivities were unspectacular.…”