Literature DB >> 22773252

Tuberculosis: finding a new potential antimycobacterium derivative in a aldehyde-arylhydrazone-oxoquinoline series.

Fernanda da C Santos1, Helena C Castro, Maria Cristina S Lourenço, Paula A Abreu, Pedro N Batalha, Anna C Cunha, Guilherme S L Carvalho, Carlos R Rodrigues, Cid A Medeiros, Simone D Souza, Vitor F Ferreira, Maria C B V de Souza.   

Abstract

Tuberculosis (TB) is a contagious disease caused by Mycobacterium tuberculosis, which remains a serious public health problem. The emergence of resistant bacterial strains has continuously increased and new treatment options are currently in need. In this work, we identified a new potential aldehyde-arylhydrazone-oxoquinoline derivative (4e) with interesting chemical structural features that may be important for designing new anti-TB agents. This 1-ethyl-N'-[(1E)-(5-nitro-2-furyl)methylene]-4-oxo-1,4-dihydroquinoline-3-carbohydrazide (4e) presented an in vitro active profile against M. tuberculosis H37Rv strain (minimum inhibitory concentration, MIC = 6.25 μg/mL) better than other acylhydrazones described in the literature (MIC = 12.5 μg/mL) and close to other antitubercular agents currently on the market. The theoretical analysis showed the importance of several structural features that together with the 5-nitro-2-furyl group generated this active compound (4e). This new compound and the analysis of its molecular properties may be useful for designing new and more efficient antibacterial drugs.

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Year:  2012        PMID: 22773252     DOI: 10.1007/s00284-012-0176-6

Source DB:  PubMed          Journal:  Curr Microbiol        ISSN: 0343-8651            Impact factor:   2.188


  29 in total

1.  Tuberculosis: medical management update.

Authors:  Juan F Yepes; Jennifer Sullivan; Andres Pinto
Journal:  Oral Surg Oral Med Oral Pathol Oral Radiol Endod       Date:  2004-09

Review 2.  Prediction of solubility and permeability class membership: provisional BCS classification of the world's top oral drugs.

Authors:  Arik Dahan; Jonathan M Miller; Gordon L Amidon
Journal:  AAPS J       Date:  2009-10-30       Impact factor: 4.009

3.  Rapid, low-technology MIC determination with clinical Mycobacterium tuberculosis isolates by using the microplate Alamar Blue assay.

Authors:  S G Franzblau; R S Witzig; J C McLaughlin; P Torres; G Madico; A Hernandez; M T Degnan; M B Cook; V K Quenzer; R M Ferguson; R H Gilman
Journal:  J Clin Microbiol       Date:  1998-02       Impact factor: 5.948

4.  Antiplatelet properties of novel N-substituted-phenyl-1,2,3-triazole-4-acylhydrazone derivatives.

Authors:  Anna C Cunha; Juliana M Figueiredo; Jorge L M Tributino; Ana L P Miranda; Helena C Castro; Russolina B Zingali; Carlos A M Fraga; Maria Cecília B V de Souza; Vitor F Ferreira; Eliezer J Barreiro
Journal:  Bioorg Med Chem       Date:  2003-05-01       Impact factor: 3.641

5.  Synthesis, characterization and antimicrobial activity of some substituted 1,2,3-triazoles.

Authors:  Bantwal Shivarama Holla; Manjathuru Mahalinga; Mari Sithambaram Karthikeyan; Boja Poojary; Padiyath Mohammed Akberali; Nalilu Suchetha Kumari
Journal:  Eur J Med Chem       Date:  2005-06-24       Impact factor: 6.514

6.  Efficient synthesis, spectral analysis and antimicrobial studies of nitrogen and sulfur containing spiro heterocycles from 2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-ones.

Authors:  M Rani; R Ramachandran; S Kabilan
Journal:  Bioorg Med Chem Lett       Date:  2010-09-15       Impact factor: 2.823

7.  Synthesis, anti-tuberculosis activity, and 3D-QSAR study of 4-(adamantan-1-yl)-2-substituted quinolines.

Authors:  Amit Nayyar; Vikramdeep Monga; Alpeshkumar Malde; Evans Coutinho; Rahul Jain
Journal:  Bioorg Med Chem       Date:  2006-11-01       Impact factor: 3.641

Review 8.  Global tuberculosis control: lessons learnt and future prospects.

Authors:  Christian Lienhardt; Philippe Glaziou; Mukund Uplekar; Knut Lönnroth; Haileyesus Getahun; Mario Raviglione
Journal:  Nat Rev Microbiol       Date:  2012-05-14       Impact factor: 60.633

9.  (E)-1-Ethyl-4-oxo-N'-(4-pyridylmethyl-ene)-1,4-dihydroquinoline-3-carbo-hydrazide.

Authors:  Fernanda da C Santos; Pedro Netto Batalha; Anna Claudia Cunha; Rafael A Alão; Vitor Francisco Ferreira; Maria Cecilia B V de Souza; Sauli Santos
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-09-16

10.  Identification of nor-β-lapachone derivatives as potential antibacterial compounds against Enterococcus faecalis clinical strain.

Authors:  André L Lourenço; Paula A Abreu; Bruno Leal; Eufrânio N da Silva Júnior; Antonio V Pinto; Maria do Carmo F R Pinto; Alessandra M T Souza; Juliana S Novais; Marcela B Paiva; Lucio M Cabral; Carlos R Rodrigues; Vitor F Ferreira; Helena C Castro
Journal:  Curr Microbiol       Date:  2010-09-30       Impact factor: 2.343

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