Literature DB >> 20623095

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

Marcelle de L Ferreira1, Raoni S B Gonçalves, Laura N de F Cardoso, Carlos R Kaiser, Andre L P Candea, Maria das Graças M de O Henriques, Maria C S Lourenço, Flavio A F M Bezerra, Marcus 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.

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Year:  2010        PMID: 20623095      PMCID: PMC5763922          DOI: 10.1100/tsw.2010.124

Source DB:  PubMed          Journal:  ScientificWorldJournal        ISSN: 1537-744X


  2 in total

1.  Anti-Mycobacterial Evaluation of 7-Chloro-4-Aminoquinolines and Hologram Quantitative Structure-Activity Relationship (HQSAR) Modeling of Amino-Imino Tautomers.

Authors:  Marcelle L F Bispo; Camilo H S Lima; Laura N F Cardoso; André L P Candéa; Flávio A F M Bezerra; Maria C S Lourenço; Maria G M O Henriques; Ricardo B Alencastro; Carlos R Kaiser; Marcus V N Souza; Magaly G Albuquerque
Journal:  Pharmaceuticals (Basel)       Date:  2017-06-09

Review 2.  In vitro anti-mycobacterial activity of (E)-N'-(monosubstituted-benzylidene) isonicotinohydrazide derivatives against isoniazid-resistant strains.

Authors:  Tatiane S Coelho; Jessica B Cantos; Marcelle L F Bispo; Raoni S B Gonçalves; Camilo H S Lima; Pedro E A da Silva; Marcus V N Souza
Journal:  Infect Dis Rep       Date:  2012-02-06
  2 in total

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