title: Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
abstract: Three classes of fused bipyridine heterocycles were designed, synthesized and evaluated for their antimycobacterial 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 mono-salt 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.
authors.affiliation: "Al. I. Cuza" University of Iasi, Organic and Biochemistry Department, Bd. Carol 11, 700506 Iasi, Romania.
authors.forename: Ramona
authors.initials: R
authors.lastname: Danac
authors.affiliation: "Al. I. Cuza" University of Iasi, Organic and Biochemistry Department, Bd. Carol 11, 700506 Iasi, Romania. Electronic address: ionelm@uaic.ro.
authors.forename: Ionel I
authors.initials: II
authors.lastname: Mangalagiu
mesh_terms: D000995:Antitubercular Agents / Q000494:pharmacology*; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D009584:Nitrogen / Q000737:chemistry*; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000995:Antitubercular Agents; D006571:Heterocyclic Compounds; D011725:Pyridines; D009584:Nitrogen
keywords: Antimycobacterial; Bipyridine; Bis-fused pyridine; LORA; MBC; MIC; MTT