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Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Preparation and in-vitro evaluation of 4-benzylsulfanylpyridine-2-carbohydrazides as potential antituberculosis
Petra Herzigová1, Vera Klimesová, Karel Palát
1Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Králové, Czech Republic.
Abstract:
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 micromol/L, most often 4 to 32 micromol/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.