title: Design, synthesis, and bioactivities screening of a diaryl ketone-inspired pesticide molecular library as derived from natural products.
abstract: Three natural products, 1,5-diphenylpentan-1-one, 1,5-diphenylpent-2-en-1-one, and 3-hydroxy-1,5-diphenylpentan-1-one, with good insecticidal activities were extracted from Stellera chamaejasme L. Based on their shared diaryl ketone moiety as 'pharmacophores', a series of diaryl ketones were synthesized and tested for insecticidal activity, acetylcholinesterase inhibitory activity, and antifungal activity. All synthesized compounds showed poor insecticidal and acetylcholinesterase inhibitory activities. Compound III with a furyl ring showed strong activities against plant pathogenic fungi. The IC(50) of compound (E)-1-(2,4-dichlorophenyl)-3-(furan-2-yl)- -prop-2-en-1-one (III(2) ) was 1.20 mg/L against Rhizoctonia solani, suggesting its strong potential as a novel antifungal drug.
authors: Institute of Applied Ecology, Chinese Academy of Sciences, Shenyang, China.
authors: Hong
authors: H
authors: Zhang
authors: Hong
authors: H
authors: Jin
authors: Lan-zhu
authors: LZ
authors: Ji
authors: Ke
authors: K
authors: Tao
authors: Wei
authors: W
authors: Liu
authors: Hao-yu
authors: HY
authors: Zhao
authors: Tai-ping
authors: TP
authors: Hou
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001042:Aphids; D001688:Biological Products / Q000302:isolation & purification*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D020128:Inhibitory Concentration 50; D007659:Ketones / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D010575:Pesticides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000935:Antifungal Agents; D001688:Biological Products; D002800:Cholinesterase Inhibitors; D007659:Ketones; D010575:Pesticides