Versatile approach to densely substituted isoxazolines and pyrazolines: Focus on a quaternary carbon center as a constitutive feature

被引：12
作者：
Abdelli, Abderrahmen [1 ]
Gharsa, Haythem [2 ]
Jmai, Momtez [1 ]
Gaucher, Anne [3 ]
Efrit, Mohamed Lotfi [1 ]
M'rabet, Hedi [1 ]
Prim, Damien [3 ]
机构：
[1] Univ Tunis El Manar, Fac Sci Tunis, Lab Synth Organ & Heterocycl Select Evaluat Activ, LR17ES01,Campus Univ, Tunis 2092, Tunisia
[2] Univ Tunis El Manar, Fac Sci Tunis, Lab Microorganismes & Biomol Actives, Tunis 2092, Tunisia
[3] Univ Paris Saclay, Inst Lavoisier Versailles, CNRS, UVSQ, F-78035 Versailles, France
来源：
TETRAHEDRON LETTERS | 2020年 / 61卷 / 23期
关键词：
1,3-Dipolar cycloaddition; Isoxazolines; Pyrazolines; Staphylococcus aureus; ANTIMICROBIAL ACTIVITY; DERIVATIVES; OXIDES; OXIDATION; CHLORIDE; BEARING; DESIGN; OXIMES; ACCESS; BETA;
D O I：
10.1016/j.tetlet.2020.151958
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A new family of isoxazolines has been obtained via 1,3-dipolar cycloaddition in good to high yields under mild conditions. Our approach focused on construction of the heterocyclic ring and direct access to a quaternary carbon center at position 5. The methodology has also been extended to pyrazoline analogues. The antibacterial activity of these compounds was evaluated, showing specific antibacterial activity against Staphylococcus aureus. Six members of these heterocycles exhibited MIC values of 4 mu g/mL. (C) 2020 Elsevier Ltd. All rights reserved.
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页数：4
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