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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Research Article

Microwave-assisted Synthesis of 2-Styrylquinoline-4-carboxylic Acids as Antitubercular Agents

Author(s): Gisela C. Muscia, Silvia E. Asis* and Graciela Y. Buldain

Volume 13, Issue 5, 2017

Page: [448 - 452] Pages: 5

DOI: 10.2174/1573406412666160901102710

Price: $65

Abstract

Background: Many 2-substituted quinolines and especially 2-arylvinyl derivatives isolated from plants or prepared by synthesis have been designed from ethnopharmacological studies.

Objective: In order to explore new aspects of the structure-antituberculosis activity relationship, a series of styrylquinoline derivatives was prepared.

Method: A series of styrylquinoline derivatives was prepared from quinaldic acid and a variety of arylbenzaldehydes under eco-friendly conditions via Knoevenagel reaction and trifluoroacetic acid (TFA) as catalyst.

Results: The products were obtained in short reaction times and good yields and were evaluated for growth inhibitory activity towards Mycobacterium tuberculosis H37Rv (Mtb) through the National Institute of Allergy and Infectious Diseases (NIAID, USA).

Conclusion: Three compounds had activity under aerobic conditions.

Keywords: Synthesis, microwave, styrylquinolines, catalysis, Mycobacterium tuberculosis, tuberculosis.

Graphical Abstract

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