Design, Synthesis and Bioactivity of Phenoxy Carboxylate(amide) Derivatives Containing 4,6-Dimethoxypyrimidine

Publisher： Bentham Science Publishers

E-ISSN： 1875-628x|14|2|228-232

ISSN： 1570-1808

Source： Letters in Drug Design & Discovery, Vol.14, Iss.2, 2016-12, pp. : 228-232

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Abstract

Aryloxy phenoxy propionic acid esters (APP) chiral herbicide is a kind of acetyl coenzymeA carboxylase enzyme (Acetyl CoA Carboxylase) inhibitor. Sulfonylureas and diphenylethersherbicide are the acetohydroxyacid synthase (ALS) inhibitors and 4,6-dimethoxypyrimidine is themajor active group. Bioisosterism and active group combination principle were the primary and effectiveways to develop novel pesticides. By using the above principles, we synthesized phenoxypropionate and phenoxy acetamide compounds which containing 4,6-dimethoxypyrimidine. Bioassayresults showed that these compounds have no obvious herbicidal activities, but some of them showedhigher inhibitory activities for cucumber downy mildew (Pseudoperonospora cubensis) and tomatolate blight (Phytophthora infestans), the individual compounds showed milder inhibitory activitiesfor wheat powdery mildew (Blumeria graminis) and rice blast (Pyricularia grisea).

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