Synthesis and Biological Evaluation of N,N′-di(thiopheneacetyl)diamines Series as Antitubercular Agents
摘要:
The series of new N,N'-di(thiopheneacetyl)diamines derivatives, 8-17, were synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis(TB), and the activity expressed as the minimum inhibitory concentration (MIC) in g/mL. Compound 13 was the only one determined to be active and exhibited a MIC 50 g/mL, indicating that the alkyl chain-length of the diamines is critical for biological activity. This class of compound has not been evaluated before, and it could be a good starting point to find new lead compounds in the fight against multi-drug resistant TB.
Synthesis and Biological Evaluation of N,N′-di(thiopheneacetyl)diamines Series as Antitubercular Agents
作者:Marcus Vinícius Nora de Souza、Maria Cristina Silva Lourenço、Mônica Amado Peralta、Raoni Schroeder Borges Gonçalves、Thais Cristina Mendonça Nogueira、Camilo Henrique da Silva Lima、Marcelle de Lima Ferreira、Emerson Teixeira da Silva
DOI:10.1080/10426500802049803
日期:2008.11.7
The series of new N,N'-di(thiopheneacetyl)diamines derivatives, 8-17, were synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis(TB), and the activity expressed as the minimum inhibitory concentration (MIC) in g/mL. Compound 13 was the only one determined to be active and exhibited a MIC 50 g/mL, indicating that the alkyl chain-length of the diamines is critical for biological activity. This class of compound has not been evaluated before, and it could be a good starting point to find new lead compounds in the fight against multi-drug resistant TB.