Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives

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 H37Rv....

Full description

Saved in:
Bibliographic Details
Main Authors: Marcelle de L. Ferreira, Raoni S.B. Gonçalves, Laura N. de F. Cardoso, Carlos R. Kaiser, Andre L.P. Candéa, Maria das Graças M. de O. Henriques, Maria C.S. Lourenço, Flávio A.F.M. Bezerra, Marcus V. N. de Souza
Format: Article
Language:English
Published: Wiley 2010-01-01
Series:The Scientific World Journal
Online Access:http://dx.doi.org/10.1100/tsw.2010.124
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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 H37Rv. 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.
ISSN:1537-744X