Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives. (2010)

• Record Type: Journal Article
• Authors: Ferreira, Marcelle de L.; Gonçalves, Raoni S.B.; Cardoso, Laura N. de F.; Kaiser, Carlos R.; Candéa, Andre L.P.; Henriques, Maria das Graças M. de O.; Lourenço, Maria C.S.; Bezerra, Flávio A.F.M.; de Souza, Marcus V. N.
• Other Names: Cos Paul Academic Editor.
• Is Part Of: TheScientificWorldjournal. Volume 10(2010)
• Page Start: 1347
• Page End: 1355
• Publication Date: 2010
• Subjects: tuberculosis -- quinoline -- isoniazid -- drugs; Science -- Periodicals; Technology -- Periodicals; Medicine -- Periodicals; 505
• DOI: 10.1100/tsw.2010.124
• Languages: English
• ISSNs: 2356-6140

Abstract

Abstract : Two series of N' (E)-heteroaromatic-isonicotinohydrazide derivatives (3a-f and 4a-b) and 1-(7-chloroquinolin-4-yl)-2-[(heteroaromatic)methylene]hydrazone derivatives (5a-f and 6a-b) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37 Rv. Several compounds were noncytotoxic and exhibited significant minimum inhibitory concentration (MIC) activity (3.12, 2.50, 1.25, or 0.60 μg/mL), which can be compared to that of the first-line drugs ethambutol (3.12 μg/mL) and rifampicin (2.0 μg/ml). These results can be considered an important starting point for the rational design of new leads for anti-TB compounds.