438565-35-6Relevant academic research and scientific papers
Synthesis, cytotoxic activity and binding model analysis of novel isoxazole-docetaxel analogues with C3′-N modification
Chen, Ming,Liu, Jiyuan,Tian, Zhen,Liu, Xueying,Zhang, Shengyong
, p. 1355 - 1365 (2018/04/10)
Structure–activity relationship (SAR) studies confirm that modifications at C-3′ position can lead to the development of highly potent novel taxoids. We designed and synthesized a series of novel isoxazole-docetaxel analogues A1–A5 by introducing isoxazol
Ultrasonic-assisted synthesis of 1,4-disubstituted 1,2,3-triazoles via various terminal acetylenes and azide and their quorum sensing inhibition
Zhang, Da-wei,Zhang, Yu-min,Li, Jing,Zhao, Tian-qi,Gu, Qiang,Lin, Feng
, p. 343 - 353 (2016/12/23)
An efficient synthesis of 1,4-disubstituted 1,2,3-triazole derivatives was studied. 1,4-Disubstituted 1,2,3-triazoles containing isoxazole and thymidine structures were synthesized in 84–96% yields starting from various terminal isoxazole ether alkynes and β-thymidine azide derivatives via a 1,3-dispolar cycloaddition using copper acetate, sodium ascorbate as the catalyst under ultrasonic assisted condition. All the target compounds were characterized by HRMS, FT-IR, 1H NMR and 13C NMR spectroscopy. Furthermore, the quorum sensing inhibitory activities of synthesized compounds were evaluated with Chromobacterium violaceum (C. Violaceum CV026) based on their inhibition of violacein production, with compound C10-HSL as a positive control. The compounds 8a, 8c and 8f exhibited considerable levels of inhibitory activity against violacein production, and IC50 values were 217?±?19, 223?±?20 and 42.8?±?4.5?μM, respectively, which highlighted the potential of these compounds as lead structures for further research towards the development of novel QS inhibitors.
A rapid and efficient solvent-free microwave-assisted synthesis of pyrazolone derivatives containing substituted isoxazole ring
Zhang, Dawei,Zhang, Yumin,Zhao, Tianqi,Li, Jing,Hou, Yaya,Gu, Qiang
, p. 2979 - 2987 (2016/05/19)
An efficient synthesis of 4-substituted pyrazolone derivatives was developed. 4-Substituted pyrazolone derivatives were synthesized in 78-97% yields starting from various 3-substituted isoxazole-5-carbaldehydes, ethyl acetoacetate and hydrazine under micr
Efficient synthesis of bis-isoxazole ethers via 1,3-dipolar cycloaddition catalysed by Zn/Zn2+ and their antifungal activities
Zhang, Da-Wei,Lin, Feng,Li, Bo-Chao,Liu, Hong-Wei,Zhao, Tian-Qi,Zhang, Yu-Min,Gu, Qiang
, p. 1500 - 1511 (2015/09/15)
An efficient method was developed for synthesising isoxazoles. A series of novel bis-isoxazole ether compounds VI, VII and VIII were synthesised starting from different substituted aldehydes (I) via a 1,3-dispolar cycloaddition using Zn/Zn2+ as a catalyst; these were characterised by FT-IR, HRMS, 1H NMR and 13C NMR spectroscopy. In addition, the antimicrobial properties of the synthesised products were investigated. The synthesised compounds exhibited significant antifungal activities in comparison with the standard drugs, fluconazole and itraconazole. It was found that Candida albicans was sensitive to 2-substituted phenyl bis-isoxazole ethers bearing pyridyl.
One-pot synthesis of (3-phenylisoxazol-5-yl) methanol derivatives under ultrasound
Shen, Chuansheng,Zhang, Yumin,Gan, Yuanming,Zhao, Tianqi,Gu, Qiang
, p. 278 - 281 (2012/04/18)
An ultrasonic-assisted, one-pot, efficient, convenient procedure for the synthesis of (3-phenylisoxazol-5-yl)methanol derivatives has been developed. (3-Phenylisoxazol-5-yl)-methanol derivatives with biological and pharmaceutical property have been synthe
Synthesis and characterization of 2-Alkyl -5-{4-[(3-nitrophenyl- 5isoxazolyl)methoxy]phenyl}-2H-tetrazoles
Mirzaei,Edjlali
experimental part, p. 685 - 694 (2010/10/20)
Heteroaryl substituted analogs of antirhnoviral (A), was prepared by a convergent approach. 3-Nitrophenyl-5bromooromethylisoxazoles 5a-b were synthesized by [3+2] cycloaddition of 3-(benzoyloxy)-propyne 2 to in situ generated arylnitrile oxides followed by deprotection of cycloadducts 3a-b and bromination of the resulting alcohols 4a-b. Coupling of 3nitrophenyl-5- bromooromethylisoxazoles (5a-b) with 4-[5-(2-alkyl-2H-tetrazolyl)]phenols (6a-d) in N-methylpyrrolidinone under mild conditions afforded a new series of 2-alkyl-5-{4-[1-(3-nitrophenyl-5-isoxazolyl)methyloxy]phenyl}-2H-tetrazoles (7a-h) in high yields. The structures of the synthesized compounds were confirmed by their 1H NMR, Mass spectral, and Elemental Analysis data.
Synthesis of isoxazolines and isoxazoles using poly(ethylene glycol) as support
Shang, Yong-Jia,Wang, Yan-Guang
, p. 1663 - 1668 (2007/10/03)
A general method for the liquid-phase syntheses of isoxazoles and isoxazolines through a 1,3-dipolar cycloaddition is described. The poly(ethylene glycol) (PEG)-supported alkyne 2 or alkene 6 reacted with nitrile oxides generated in situ from aldoximes 3, followed by cleavage from the PEG, to give isoxazoles or isoxazolines in good yield and purity.
Soluble polymer-supported synthesis of isoxazoles
Shang, Yong-Jia,Wang, Yan-Guang
, p. 2247 - 2249 (2007/10/03)
The first soluble polymer-supported synthesis of isoxazoles through a 1,3-dipolar cycloaddition is described. A soluble polymer-supported alkyne reacts with nitrile oxides generated in situ to give isoxazoles in good yield.
