Salicylanilide carbamates: antitubercular agents active against multidrug-resistant Mycobacterium tuberculosis strains

Bioorg Med Chem. 2010 Feb;18(3):1054-61. doi: 10.1016/j.bmc.2009.12.055.

Juana M Férriz ¹, Katerina Vávrová, Filip Kunc, Ales Imramovský, Jirina Stolaríková, Eva Vavríková, Jarmila Vinsová

Affiliations

Affiliation

1 Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.

PMID: 20060303 DOI: 10.1016/j.bmc.2009.12.055

Abstract

A series of 27 salicylanilide-based carbamates was prepared as a part of our ongoing search for new antituberculosis drugs. These compounds exhibited very good in vitro activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium and, in particular, against five multidrug-resistant strains, with MIC values between 0.5-2 micromol/L. Moreover, they displayed moderate toxicity against intestinal cells with the selectivity index being up to 96. Furthermore, acid stability and a half-life of 43h at pH 7.4 were shown. Thus, these novel salicylanilide derivatives are drug candidates which should be seriously consider for further screening.

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