The synthesis and antimycobacterial properties of 4-(substituted benzylsulfanyl)pyridine-2-carboxamides
4-(Substituted benzylsulfanyl)pyridine-2-carboxamides 6 were synthesized by a three-step synthesis starting from 4-chloropyridine-2-carboxylic acid and substituted benzyl thiols, with the exception of nitroderivatives. The compounds were evaluated for their anti-TB activity against M. tuberculosis, non-tuberculous mycobacteria (M. kansasii and M. avium), and MDR strains of M. tuberculosis. The activities expressed as the minimum inhibitory concentration (MIC) fall into the range of 8-250 μmol/L. The substances exhibited similar activities against both sensitive and resistant strains. ARKAT-USA, Inc.
Preparation and in-vitro evaluation of 4-benzylsulfanylpyridine-2- carbohydrazides as potential antituberculosis agents
A set of 4-benzylsulfanylpyridine-2-carbohydrazides was synthesized and evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis, non-tuberculous mycobacteria, and multidrug-resistant M. tuberculosis. The activities expressed as the minimum inhibitory concentration (MIC) fall into a range of 2 to 125 μmol/L, most often 4 to 32 μmol/L. The results revealed that the substituents on the benzyl moiety do not influence the antimycobacterial efficacy. The substances exhibited similar activities against sensitive and resistant strains of M. tuberculosis. Furthermore, compounds show low antiproliferative effect and cytotoxicity.