61096-86-4Relevant academic research and scientific papers
Potassium iodate (KIO 3) as a novel reagent for the synthesis of isoxazolines: evaluation of antimicrobial activity of the products
Kotian, Sumana Y,Abishad,Byrappa,Rai, K M Lokanatha
, (2019/05/28)
Abstract : A novel reagent for the synthesis of isoxazolines has been reported. Aryl aldoximes were made to react with alkenes in the presence of KIO 3 as the oxidising agent. This new reagent has been useful as an oxidant in the synthesis of i
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.
Pyrazole and Isoxazole Derivatives as New, Potent, and Selective 20-Hydroxy-5,8,11,14-eicosatetraenoic Acid Synthase Inhibitors
Nakamura, Toshio,Sato, Masakazu,Kakinuma, Hiroyuki,Miyata, Noriyuki,Taniguchi, Kazuo,Bando, Kagumi,Koda, Ayumi,Kameo, Kazuya
, p. 5416 - 5427 (2007/10/03)
In a previous paper, we reported the N-hydroxyformamidine derivative HET0016 as a potent and selective 20-HETE synthase inhibitor. Despite its attraction as a potential therapeutic agent for cerebral diseases, the preparation of an injectable formulation
A NEW SERIES OF MESOGENIC DERIVATIVES OF PYRIMIDINE-SUBSTITUTED 2-(O-HYDROXYPHENYL)PYRIMIDINES
Mikhaleva, M. A.,Bolotin, B. M.,Serebryakova, E. S.,Safina, R. U.,Kizner, T. A.,Sklyarova, E. G.
, p. 316 - 320 (2007/10/02)
Analogs of known mesogenic 2,5-diarylpyrimidines, 5--2-(o-hydroxy-p-alkoxyphenyl)pyrimidines (I), have been synthesized that have a wider mesogenic phase temperature range.Pyrimidines I show smectic C and A phases but not the nemati
Structure-activity analysis of a class of orally active hydroxamic acid inhibitors of leukotriene biosynthesis
Summers,Gunn,Martin,Martin,Mazdiyasni,Stewart,Young,Bouska,Dyer,Brooks,Carter
, p. 1960 - 1964 (2007/10/02)
The nature of the carbonyl and nitrogen substituents of hydroxamic acids has a major influence on the biological profile of these compounds. Hydroxamates with small groups such as methyl appended to the carbonyl and relatively large nitrogen substituents
