Synthesis and antitubercular activity of heteroaromatic isonicotinoyl and 7-chloro-4-quinolinyl hydrazone derivatives.

TheScientificWorldJournal
Marcelle de L FerreiraMarcus V N de Souza

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 H37Rv. Several compounds were noncytotoxic and exhibited significant minimum inhibitory concentration (MIC) activity (3.12, 2.50, 1.25, or 0.60 microg/mL), which can be compared to that of the first-line drugs ethambutol (3.12 microg/mL) and rifampicin (2.0 microg/ml). These results can be considered an important starting point for the rational design of new leads for anti-TB compounds.

Citations

Mar 26, 2015·Journal of Enzyme Inhibition and Medicinal Chemistry·Pedro Henrique de Azambuja CarvalhoRafael Guerra Lund
Jan 29, 2013·Chemical Biology & Drug Design·Elaine S CoimbraMarcus V N de Souza
Mar 13, 2014·Archiv der Pharmazie·Laura N F CardosoMarcus V N de Souza
Feb 16, 2019·Journal of Biomolecular Structure & Dynamics·Porkodi JeyaramanRaman Natarajan
Aug 28, 2021·Natural Product Research·Irina E SmirnovaOxana B Kazakova

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