4058-91-7Relevant articles and documents
Pyrazolopyrimidinone compound and preparation method and application thereof
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Paragraph 0067; 0073; 0079; 0085; 0091; 0097; 0103; 0109, (2019/08/26)
The invention belongs to the technical field of herbicides and particularly relates to a pyrazolopyrimidinone compound and a preparation method and application thereof. The provided pyrazolopyrimidinone compound shows good herbicidal activity on four tested plants (rape, amaranth, barnyard grass and crab grass) at the dosage of 1,500 gram/hectare, and a compound 4 and a compound 7 achieve the nearly 100% inhibition rate on the four tested plants (rape, amaranth, barnyard grass and crab grass). At the same time, the dosages of the compounds 4 and 7 are reduced for a herbicidal activity test, and the compound 7 still shows great herbicidal activity at the dosage of 93.75 gram/hectare. The pyrazolopyrimidinone compound has a very great application prospect.
PF-04859989 as a template for structure-based drug design: Identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency
Dounay, Amy B.,Anderson, Marie,Bechle, Bruce M.,Evrard, Edelweiss,Gan, Xinmin,Kim, Ji-Young,McAllister, Laura A.,Pandit, Jayvardhan,Rong, Suobao,Salafia, Michelle A.,Tuttle, Jamison B.,Zawadzke, Laura E.,Verhoest, Patrick R.
, p. 1961 - 1966 (2013/04/23)
The structure-based design, synthesis, and biological evaluation of a new pyrazole series of irreversible KAT II inhibitors are described herein. The modification of the inhibitor scaffold of 1 and 2 from a dihydroquinolinone core to a tetrahydropyrazolopyridinone core led to discovery of a new series of potent KAT II inhibitors with excellent physicochemical properties. Compound 20 is the most potent and lipophilically efficient of these new pyrazole analogs, with a kinact/Ki value of 112,000 M-1 s -1 and lipophilic efficiency (LipE) of 8.53. The X-ray crystal structure of 20 with KAT II demonstrates key features that contribute to this remarkable potency and binding efficiency.
Novel protoporphyrinogen oxidase inhibitors: 3H-pyrazolo[3,4-d][1,2,3] triazin-4-one derivatives
Li, Hua-Bin,Zhu, You-Quan,Song, Xiao-Wei,Hu, Fang-Zhong,Liu, Bin,Li, Yong-Hong,Niu, Zi-Xia,Liu, Pei,Wang, Zhi-Hong,Song, Hai-Bin,Zou, Xiao-Mao,Yang, Hua-Zheng
experimental part, p. 9535 - 9542 (2010/03/31)
A series of 3H-pyrazolo[3,4-d][1,2,3]triazin-4-one derivatives were synthesized as candidate herbicides by diazotization of different 5(3)-amino-N-phenyl-1H-pyrazole-4-carboxamide derivatives prepared by the reaction of substituted 5(3)-amino-pyrazole-4-carbonyl chloride with a substituted aniline. Their structures were identified by 1H NMR and elemental analyses. The isomers D and E were isolated, and their structures were identified by two-dimensional NMR analyses (heteronuclear single quantum coherence and heteronuclear multiple-bond correlation) and single-crystal X-ray diffraction analysis. The bioassay results showed that some of the title compounds exhibited both excellent herbicidal activity at a dose of 93.75 g/ha and strong inhibition against protoporphyrinogen oxidase activity in vitro. The structure-activity relationship showed that D16 possessed the highest activities both in vivo and in vitro when the N-substituted group of the pyrazole ring was allyl and the N-substituted group of benzooxazinone was propargyl.