Synthesis and Antibacterial Activities of 2---phenylacetamide Derivatives Containing a Dissulfone Moiety Target on Clp.

J Agric Food Chem

State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, China.

Published: August 2022

Rice bacterial blight and rice bacterial streak are two serious rice diseases and have caused great harm to the production of rice all over the world. To develop an efficient antibacterial agent with a novel target, a series of novel 2---phenylacetamide derivatives containing a dissulfone moiety were synthesized, and their antibacterial activities were evaluated. Among them, compound exhibited the best antibacterial activities, especially against and with EC values of 0.63 and 0.79 mg/L, respectively, which were much better than the commercial control of bismerthiazol () (76.59 and 83.35 mg/L, respectively) and thiodiazole copper () (91.72 and 114.00 mg/L, respectively). Meanwhile, compound can interact with a CRP-like protein (Clp) of Pxo99 and show strong binding activity with -Clp with a value of 0.52 μM, which was far superior to the corresponding values of (183.94 μM) and (222.58 μM). Treatment of and deletion of the gene could significantly reduce the expression of the gene and attenuate the virulence of pathogenic bacteria. These results indicated that compound could be used as a potential novel agricultural bactericide and Clp can be used as a target protein for the control of plant bacterial diseases. This work provided reliable support for developing novel antibacterial agents based on Clp as a target protein.

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Source
http://dx.doi.org/10.1021/acs.jafc.2c02605DOI Listing

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