Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 74, Issue -, Pages 664-670Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.09.061
Keywords
Antimycobacterial; Bipyridine; Bis-fused pyridine; MIC; MBC; LORA; MIT
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Funding
- CNCSIS Bucuresti, Romania [PN-II-DE-PCE-2011-3-0038, 268/05.10.2011]
- National Institutes of Health and the National Institute of Allergy and Infectious Diseases [HHSN272201100012I]
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Three classes of fused bipyridine heterocycles were designed, synthesized and evaluated for their anti-mycobacterial activities. The method for preparation of fused bipyridine derivatives is straight and efficient. The primary antimycobacterial screening reveals that mono-indolizine mono-salts are displaying potency superior to the second-line antitubercular drugs Cycloserine and Pyrimethamine and, equal as the first line anti-TB Ethambutol. The data from Cycle-2 screening assay (MIC, MBC, LORA, intracellular (macrophage) drug screening, and MTT cell proliferation) confirm the promising anti-TB results from Cycle-1 for mono-indolizine mono-salts. These data indicate that mono-indolizine monosalt 6d is a potent compound against both replicating and non-replicating Mycobacterium tuberculosis, is active against both extracellular and intracellular organisms, has a bacteriostatic mechanism of action and has basically no toxicity. We see no influence concerning the anti-TB activity of the fused-pyridine substituents. (C) 2013 Elsevier Masson SAS. All rights reserved.
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