221559-20-2Relevant academic research and scientific papers
Discovery of novel 3-{[(5,5-dimethyl-4,5-dihydroisoxazol-3-yl)sulfonyl]methyl}benzo[d]isoxazole analogs as promising very long chain fatty acids inhibitors
Lin, Jian,Li, Yitao,Hu, Xiaoyun,Chi, Weilin,Zeng, Shuiming,Xu, Junxing
, p. 226 - 240 (2020/10/19)
Very long chain fatty acids (VLCFAs) are one of the most principal and promising targets for herbicides discovery. In order to explore and find novel VLCFAs inhibitors with higher herbicidal activity and improved crop safety, a variety of new 3-{[(5,5-dimethyl-4,5-dihydroisoxazol-3-yl)sulfonyl]methyl}benzo[d]isoxazole derivatives were reasonably designed and synthesized. The results of greenhouse experiments indicated that several compounds exhibited good herbicidal activity against Digitaria sanguinalis, Echinochloa crus-galli, and Setaria faberii at rates of 150 g ai/ha. Compounds g4 and h1 displayed promising herbicidal activity against D sanguinalis and E crus-galli at rates of 75 g ai/ha, which is better than commercial pyroxasulfone and S-metolachlor. Moreover, compound h1 displayed higher activity against E crus-galli, D sanguinalis, and S faberii than pyroxasulfone and S-metolachlor even at a rate of 37.5 and 18.75 g ai/ha. Furthermore, both of the compounds g4 and h1 were much safer to these tested crops, especially to rice, wheat and rape, at the rate of 150 g ai/ha than pyroxasulfone. Therefore, h1 may act as a new lead structure for novel herbicides discovery.
5-6-5 azatricyclic compound and preparation method thereof
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, (2019/10/01)
The embodiment of the invention discloses a preparation method of a 5-6-5 azatricyclic compound. By using 3-fluorophenol as a raw material and through multistep cascade reactions including esterification, rearrangement, oximation, intramolecular cyclizati
ISOXAZOLINE DERIVATIVES AND THEIR USES IN AGRICULTURE RELATED APPLICATION
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Paragraph 00209, (2019/04/26)
The present invention provides isoxazoline derivatives and uses thereof in agriculture; in particular, the present invention provides a compound having formula (I), or a stereoisomer, an N-oxide or a salt thereof, preparation methods thereof, and compositions containing these compounds and uses thereof in agriculture, particularly uses as herbicide active ingredients for controlling unwanted plants; wherein R1, R2, R3, R4, n, R5, R6 and Hy are as described in the invention.
Structure-Based Discovery and Optimization of Benzo [d] isoxazole Derivatives as Potent and Selective BET Inhibitors for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC)
Zhang, Maofeng,Zhang, Yan,Song, Ming,Xue, Xiaoqian,Wang, Junjian,Wang, Chao,Zhang, Cheng,Li, Chenchang,Xiang, Qiuping,Zou, Lingjiao,Wu, Xishan,Wu, Chun,Dong, Baijun,Xue, Wei,Zhou, Yulai,Chen, Hongwu,Wu, Donghai,Ding, Ke,Xu, Yong
, p. 3037 - 3058 (2018/04/23)
The bromodomain and extra-terminal (BET) family proteins have gained increasing interest as drug targets for treatment of castration-resistant prostate cancer (CRPC). Here, we describe the design, optimization, and evaluation of benzo[d]isoxazole-containing compounds as potent BET bromodomain inhibitors. Cocrystal structures of the representative inhibitors in complex with BRD4(1) provided solid structural basis for compound optimization. The two most potent compounds, 6i (Y06036) and 7m (Y06137), bound to the BRD4(1) bromodomain with Kd values of 82 and 81 nM, respectively. They also exhibited high selectivity over other non-BET subfamily members. The compounds potently inhibited cell growth, colony formation, and the expression of AR, AR regulated genes, and MYC in prostate cancer cell lines. Compounds 6i and 7m also demonstrated therapeutic effects in a C4-2B CRPC xenograft tumor model in mice. These potent and selective BET inhibitors represent a new class of compounds for the development of potential therapeutics against CRPC.
7-[2-[4-(6-fluoro-3-methyl-1,2-benzisoxazol-5-YL)-1-piperazinyl]ethyl]-2-(1-propynyl)-7H-pyrazolo-[4,3-e]-[1,2,4]-triazolo-[1,5-c]-pyrimidin-5amine
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Page/Page column 4-5, (2008/06/13)
The compound having the structural formula I or a pharmaceutically acceptable salt thereof, is disclosed, as well as its use in the treatment of central nervous system diseases, in particular Parkinson's disease, Extra Pyramidal Syndrome, restless legs syndrome and attention deficit hyperactivity disorder, pharmaceutical compositions comprising it, and combinations with other agents.
PROCESS FOR THE PREPARATION OF 6-(PERFLUOROALKYL)URACIL COMPOUNDS FROM CARBAMATE COMPOUNDS
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Page 34, (2010/02/06)
An improved process for the preparation of 6-(perfluoroalkyl)uracil compounds having structural formula (I) from carbamate compounds having structural formula (II).
