6119-12-6Relevant articles and documents
Design, synthesis, and fungicidal activity of novel 1,3,4-oxadiazole derivatives
Yu, Fuqiang,Guan, Aiying,Li, Mengru,Hu, Lan,Li, Xiaowu
, p. 915 - 918 (2018)
Employing the intermediate derivatization method (IDM), twenty novel 1,3,4-oxadiazole derivatives containing arylpyrazoloxyl moiety were designed and synthesized. The structures of the title compounds were identified by 1H NMR, 13C NMR, MS and elemental analyses, compound 4 was further identified by single-crystal X-ray diffraction. Antifungal activities against rice sheath blight (RSB) and sorghum anthracnose (SA) were evaluated by the mycelium linear growth rate method. Compounds 4, 16 and 20 displayed significant activities against RSB (EC50 = 0.88 mg/L, 0.91 mg/L and 0.85 mg/L, respectively), higher than the reference tebuconazole; While compound 3 exhibited higher activity against SA (EC50 = 1.03 mg/L), equal to commercial pyraclostrobin (EC50 = 1.06 mg/L). The study showed that compound 20 is a promising fungicide for further development.
Preparation method of 1-(4-chlorphenyl)-2H-pyrazoline-3-ketone
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Paragraph 0045-0058, (2022/03/27)
The invention relates to a preparation method of 1-(4-chlorphenyl)-2H-pyrazoline-3-ketone, an intermediate reacts with hydrogen peroxide under the action of alkali and a catalyst to generate the 1-(4-chlorphenyl)-2H-pyrazoline-3-ketone, and the structural formula of the intermediate is that the feeding molar ratio of the intermediate to the catalyst is 1: (0.0001-0.001). The preparation method of the 1-(4-chlorphenyl)-2H-pyrazoline-3-ketone has the advantages of simplicity in operation, low catalyst dosage, few three wastes, high efficiency and high yield, and is suitable for industrial production.
COMPOUND HAVING BET INHIBITORY ACTIVITY AND PREPARATION METHOD AND USE THEREFOR
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Paragraph 0196-0197, (2020/12/22)
The invention relates to the field of pharmaceutical chemistry. Specifically, the present invention relates to a series of BET (bromodomain and extra-terminal domain) inhibitors having a novel structure, particularly inhibitors targeting BRD4 (Bromodomain-containing protein 4), and a preparation method and use therefor. The structure thereof is shown in the following general formula (I). Said compounds or a stereoisomer, racemate, geometric isomer, tautomer, prodrug, hydrate, solvate, or crystal form thereof, or a pharmaceutically acceptable salt thereof, and the pharmaceutical compsosition thereof can be used for the treatment and/or prevention of related diseases mediated by bromodomain proteins.