title: Antitubercular activity of new coumarins.
abstract: The present article describes a series of 21 N '-benzylidene-2-oxo-2H-chromene-3-carbohydrazides 4a-4v, which were synthesized and evaluated for their cell viabilities in non-infected and Mycobacterium bovis Bacillus Calmette-Guerin-infected macrophages. Subsequently, the non-cytotoxic compounds 4c, 4g, 4h, 4j, 4l and 4t were assessed against Mycobacterium tuberculosis ATCC 27294 using the microplate Alamar Blue assay and the activity expressed as the minimum inhibitory concentration in μg/mL. These compounds exhibited a significant activity (50-100 μg/mL) when compared to the first-line drugs, such as pyrazinamide (PZA >100 μg/mL). These results could be considered a good starting point for further studies to develop new lead compounds to treat multidrug-resistant tuberculosis.
authors.affiliation: Universidade Federal de Alagoas, Campus Arapiraca, Rua Manoel Severino Barbosa s/n, Bonsucesso, Arapiraca, AL, Brazil.
authors.forename: Silvia H
authors.initials: SH
authors.lastname: Cardoso
authors.forename: Milena B
authors.initials: MB
authors.lastname: Barreto
authors.forename: Maria C S
authors.initials: MC
authors.lastname: Lourenço
authors.forename: Maria das Graças M de O
authors.initials: Md
authors.lastname: Henriques
authors.forename: André L P
authors.initials: AL
authors.lastname: Candéa
authors.forename: Carlos R
authors.initials: CR
authors.lastname: Kaiser
authors.forename: Marcus V N
authors.initials: MV
authors.lastname: de Souza
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000737:chemistry* / Q000494:pharmacology*; D002417:Cattle; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D003374:Coumarins / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D006835:Hydrazones / Q000737:chemistry / Q000494:pharmacology; D008264:Macrophages / Q000382:microbiology; D009163:Mycobacterium bovis / Q000187:drug effects*; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D014376:Tuberculosis / Q000188:drug therapy*; D014380:Tuberculosis, Bovine / Q000188:drug therapy
chemical_list: D000995:Antitubercular Agents; D003374:Coumarins; D006835:Hydrazones