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Infectious Disease Reports
Volume 4
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Article

In Vitro Anti-Mycobacterial Activity of (E)-N´-(Monosubstituted-benzylidene) Isonicotinohydrazide Derivatives against Isoniazid-Resistant Strains

by
Tatiane S. Coelho
1,
Jessica B. Cantos
1,
Marcelle L.F. Bispo
2,3,
Raoni S.B. Gonçalves
2,3,
Camilo H.S. Lima
2,3,
Pedro E.A. da Silva
1 and
Marcus De Souza
2,3,*
1
Universidade Federal do Rio Grande, Rio Grande do Sul, RS, Brazil
2
Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos- Far Manguinhos, Brazil
3
Universidade Federal do Rio de Janeiro, Instituto de Química, Departamento de Química Orgânica, RS, Brazil
*
Author to whom correspondence should be addressed.
Infect. Dis. Rep. 2012, 4(1), e13; https://doi.org/10.4081/idr.2012.e13
Submission received: 4 August 2011 / Revised: 3 October 2011 / Accepted: 28 October 2011 / Published: 6 February 2012

Abstract

A series of twenty-three N-acylhydrazones derived from isoniazid (INH 1-23) have been evaluated for their in vitro antibacterial activity against INH- susceptible strain of M. tuberculosis (RG500) and three INH-resistant clinical isolates (RG102, RG103 and RG113). In general, derivatives 4, 14, 15 and 16 (MIC=1.92, 1.96, 1.96 and 1.86 mM, respectively) showed relevant activities against RG500 strain, while the derivative 13 (MIC=0.98 mM) was more active than INH (MIC=1.14 mM). However, these derivatives were inactive against RGH102, which displays a mutation in the coding region of inhA. These results suggest that the activities of these compounds depend on the inhibition of this enzyme. However, the possibility of other mechanisms of action cannot be excluded, since compounds 2, 4, 6, 7, 12-17, 19, 21 and 23 showed good activities against katG-resistant strain RGH103, being more than 10-fold more active than INH.
Keywords: tuberculosis; isoniazid; INH-resistance; N-acylhydrazones; drugs tuberculosis; isoniazid; INH-resistance; N-acylhydrazones; drugs

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MDPI and ACS Style

Coelho, T.S.; Cantos, J.B.; Bispo, M.L.F.; Gonçalves, R.S.B.; Lima, C.H.S.; da Silva, P.E.A.; De Souza, M. In Vitro Anti-Mycobacterial Activity of (E)-N´-(Monosubstituted-benzylidene) Isonicotinohydrazide Derivatives against Isoniazid-Resistant Strains. Infect. Dis. Rep. 2012, 4, e13. https://doi.org/10.4081/idr.2012.e13

AMA Style

Coelho TS, Cantos JB, Bispo MLF, Gonçalves RSB, Lima CHS, da Silva PEA, De Souza M. In Vitro Anti-Mycobacterial Activity of (E)-N´-(Monosubstituted-benzylidene) Isonicotinohydrazide Derivatives against Isoniazid-Resistant Strains. Infectious Disease Reports. 2012; 4(1):e13. https://doi.org/10.4081/idr.2012.e13

Chicago/Turabian Style

Coelho, Tatiane S., Jessica B. Cantos, Marcelle L.F. Bispo, Raoni S.B. Gonçalves, Camilo H.S. Lima, Pedro E.A. da Silva, and Marcus De Souza. 2012. "In Vitro Anti-Mycobacterial Activity of (E)-N´-(Monosubstituted-benzylidene) Isonicotinohydrazide Derivatives against Isoniazid-Resistant Strains" Infectious Disease Reports 4, no. 1: e13. https://doi.org/10.4081/idr.2012.e13

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