An efficient synthesis of isoxazoline libraries of thiophene analogs and its antimycobacterial investigation (original) (raw)

Medicinal Chemistry Research, 2014

Abstract

ABSTRACT Synthesis of novel thiophene substituted isoxazoline libraries is currently of high interest. Here, we have reported detailed syntheses of 2,5-dichlorothiophene, 5-chloro-2-(benzylthio)thiophene, and 5-chlorothiophene-2-sulphonamide substituted analogs of isoxazoline from chalcones catalyzed by NaOH in PEG-400 as green solvent. In vitro antimycobacterial and antimicrobial activity of newly synthesized compounds were investigated. Compounds 2j, 2k, and 2l showed excellent activity against Mycobacterium tuberculosis and other Mycobacterium strains tested. Compounds 2a–2c, 2i showed excellent activity against all bacterial and fungal species tested. The isoxazoline scaffold synthesized in the present study may be useful in the development of novel new antimicrobial agents. Graphical abstract An efficient synthesis of isoxazoline libraries of thiophene analogs and its antimycobacterial investigation.

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