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.
Medicinal Chemistry
Title:Microwave-assisted Synthesis of 2-Styrylquinoline-4-carboxylic Acids as Antitubercular Agents
Volume: 13 Issue: 5
Author(s): Gisela C. Muscia, Silvia E. Asis*Graciela Y. Buldain
Affiliation:
- Facultad de Farmacia y Bioquímica, Departamento de Química Orgánica, Universidad de Buenos Aires, Junín 956, C1113AAB Ciudad Autónoma de Buenos Aires,Argentina
Keywords: Synthesis, microwave, styrylquinolines, catalysis, Mycobacterium tuberculosis, tuberculosis.
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.Export Options
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Cite this article as:
Muscia C. Gisela, Asis E. Silvia*, Buldain Y. Graciela, Microwave-assisted Synthesis of 2-Styrylquinoline-4-carboxylic Acids as Antitubercular Agents, Medicinal Chemistry 2017; 13 (5) . https://dx.doi.org/10.2174/1573406412666160901102710
DOI https://dx.doi.org/10.2174/1573406412666160901102710 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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