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

TETRAHEDRON LETTERS

卷:61

Article

Abdelli, Abderrahmen¹  Gharsa, Haythem²  Jmai, Momtez¹  Gaucher, Anne³  Efrit, Mohamed Lotfi¹  M'rabet, Hedi¹  Prim, Damien³ 

[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

关键词: 1,3-Dipolar cycloaddition;    Isoxazolines;    Pyrazolines;    Staphylococcus aureus;   

DOI  :  10.1016/j.tetlet.2020.151958

来源: Elsevier

【 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.

【 授权许可】

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