81465-76-1Relevant academic research and scientific papers
Synthesis of isoxazoles via cyclization of β-fluoro enones with sodium azide
Li, Liangkui,Huang, Shiqing,Mao, Kuantao,Lv, Leiyang,Li, Zhiping
, (2021/04/22)
A practical method for the synthesis of 3,5-disubstituted isoxazoles via cyclization of β-fluoro enones with sodium azide was disclosed. Density functional theory (DFT) calculation indicated that both (1) the azirine formation followed by intramolecular rearrangement and (2) direct enolate O-attack via 5-exo-trig cyclization of vinyl azide were possible for the isoxazole formation.
Development of a continuous flow photoisomerization reaction converting isoxazoles into diverse oxazole products
Bracken, Cormac,Baumann, Marcus
, p. 2607 - 2617 (2020/03/11)
A continuous flow process is presented, which directly converts isoxazoles into their oxazole counterparts via a photochemical transposition reaction. This results in the first reported exploitation of this transformation to establish its scope and synthe
Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators
Bi, Fangchao,Song, Di,Zhang, Nan,Liu, Zhiyang,Gu, Xinjie,Hu, Chaoyu,Cai, Xiaokang,Venter, Henrietta,Ma, Shutao
, p. 90 - 103 (2018/10/04)
Antibiotic resistance among clinically significant bacterial pathogens is becoming a prevalent threat to public health, and new antibacterial agents with novel mechanisms of action hence are in an urgent need. Utilizing computational docking method and structure-based optimization strategy, we rationally designed and synthesized two series of isoxazol-3-yl- and isoxazol-5-yl-containing benzamide derivatives that targeted the bacterial cell division protein FtsZ. Evaluation of their activity against a panel of Gram-positive and -negative pathogens revealed that compounds B14 and B16 that possessed the isoxazol-5-yl group showed strong antibacterial activity against various testing strains, including methicillin-resistant Staphylococcus aureus and penicillin-resistant S. aureus. Further molecular biological studies and docking analyses proved that the compound functioned as an effective inhibitor to alter the dynamics of FtsZ self-polymerization via a stimulatory mechanism, which finally terminated the cell division and caused cell death. Taken together, these results could suggest a promising chemotype for development of new FtsZ-targeting bactericidal agent.
5-PHENYL-ISOXAZOLE-3-CARBOXAMIDE DERIVATIVES AS TRPV1 MODULATORS
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Page/Page column 58, (2009/03/07)
The present invention relates to isoxazole-3-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide de
1-Benzoyl-3-(isoxazolyl or benzisoxazolyl)-ureas and insecticidal use thereof
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, (2008/06/13)
The present invention is directed to 1-(benzoyl)-3-(isoxazolyl or benzisoxazolyl)urea or thiourea compounds useful as insecticides.
