Letters in Drug Design & Discovery

Author(s): Ivan Neves Junior, Maria C.S. Lourenco, Guilherme de B.P. de Miranda, Thatyana R.A. Vasconcelos, Karla C. Pais, Jose dos P. de A. Junior, M. S.V. Wardell, James L. Wardell and V. N. de Souza

DOI: 10.2174/157018006777805549

Synthesis and In Vitro Anti-Tubercular Activity of a Series of N- (Disubstitutedbenzoyl)Isoniazid Derivatives

Page: [424 - 428] Pages: 5

  • * (Excluding Mailing and Handling)

Abstract

A series of eight N-(disubstitutedbenzoyl)isoniazid derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv using the alamar blue susceptibility test and the activity expressed as the minimum inhibitory concentration (MIC) in μg/mL. Compounds 15 and 16 exhibited a significant activity (0.5 μg/mL) when compared with first line drugs such as isoniazid (INH) and rifampicin (RIP) and could be a good starting point to develop new lead compounds in the fight against multi-drug resistant tuberculosis.

Keywords: Isoniazid, analogs, anti-tubercular activity