Synthesis and Biological Evaluation of N,N'-di(thiopheneacetyl)diamines Series as Antitubercular Agents

Authors: De Souza, M.V.N.; Lourenço, M.C.S.; Peralta, M.A.; Gonçalves, R.S.B.; Nogueira, T.C.M.; Lima, C.H.S.; Ferreira, M.L.; Silva, E.T.


Abstract

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 μ g/mL. Compound 13 was the only one determined to be active and exhibited a MIC 50 μg/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.
Keywords:Antimycobacterial activity, thiophene, tuberculosis (TB) Document Type: Research Article DOI: http://dx.doi.org/10.1080/10426500802049803 Publication date: 3 de Novembro de 2008

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