Design, synthesis and biological evaluation of novel isoniazid derivatives with potent antitubercular activity
- Autores: Aires-de-Sousa J, Correia HE, Elvas-Leitao R, Kovalishyn V, Latino DARS, Martins F, Miranda V, Ramos J, Reis M, Santos L, Santos S, Ventura C, Vitorino S, Viveiros M
- Ano de Publicação: 2014
- Journal: European Journal of Medicinal Chemistry
- Link: http://www.sciencedirect.com/science/article/pii/S0223523414004061
The disturbing emergence of multidrug-resistant strains of Mycobacterium tuberculosis(Mtb) has been driving the scientific community to urgently search for new and efficient antitubercular drugs. Despite the various drugs currently under evaluation, isoniazid is still the key and most effective component in all multi-therapeutic regimens recommended by the WHO. This paper describes the QSAR-oriented design, synthesis and in vitro antitubercular activity of several potent isoniazid derivatives (isonicotinoyl hydrazones and isonicotinoyl hydrazides) against H37Rv and two resistant Mtb strains.