Synthesis and biological evaluation of N-(aryl)-2-thiophen-2-ylacetamides series as a new class of antitubercular agents

The present article describes a series of 21 N-(aryl)-2-thiophen-2-ylacetamides, which were synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis. The present article describes a series of 21 N-(aryl)-2-thiophen-2-ylacetamides, which were synthesized...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-12, Vol.17 (24), p.6895-6898
Main Authors: Lourenço, Maria Cristina Silva, Vicente, Felipe Rodrigues, Henriques, Maria das Graças Muller de Oliveira, Peixoto Candéa, André Luis, Borges Gonçalves, Raoni Schroeder, Nogueira, Thais Cristina M., de Lima Ferreira, Marcelle, Nora de Souza, Marcus Vinícius
Format: Article
Language:English
Subjects:
Acetamides - chemical synthesis
Acetamides - chemistry
Acetamides - classification
Acetamides - pharmacology
Animals
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antimycobacterial activity
Antitubercular Agents - chemical synthesis
Antitubercular Agents - chemistry
Antitubercular Agents - classification
Antitubercular Agents - pharmacology
Biological and medical sciences
Cell Line
Macrophages - drug effects
Medical sciences
Mice
Molecular Structure
Mycobacterium tuberculosis
Pharmacology. Drug treatments
Structure-Activity Relationship
Thiopheneacetamides
Thiophenes - chemistry
Tuberculosis
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Summary:The present article describes a series of 21 N-(aryl)-2-thiophen-2-ylacetamides, which were synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis. The present article describes a series of 21 N-(aryl)-2-thiophen-2-ylacetamides, which were synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis, and the activity expressed as the minimum inhibitory concentration (MIC) in μg/mL. The compounds 2, 3, 7, 8, 11, 12, 15, 16, and 20 exhibited activity between 25 and 100 μg/mL and could be a good start point to find new lead compounds in the fight against multidrug resistant tuberculosis.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.09.096