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2. Antimicrobial evaluation of quinones and heterocyclic compounds against mycobacterium marinum, M. kansasii and M. abscessus

Author

Cantos, Jessica B., Coelho, Tatiane S., Carneiro, Paula F., Moura, Kelly C. G., Pinto, Maria Do C. F. R., Da Silva Junior, Eufranio N., and Da Silva, Pedro E. A.

Subjects
Compuestos Heterocíclicos, Antimycobacterial activity, Susceptibility, Mycobacterium kansasii, Quinones, Mycobacterium marinum, bacteria, REMA, Quinonas, bacterial infections and mycoses, Farmacia, MNT
Abstract

The resistance to antimicrobials and biocides observed in mycobacteria which do not cause tuberculosis (MNT) determines the necessity to develop drugs. The present study evaluated the activity of naphthoquinones and heterocyclic derivatives obtained from lapachol against Mycobacterium kansasii, M. marinum, and M. abscessus, through the REMA method. It was observed that lapachol was inactive against the three mycobateria species, while β-lapachone and nor-β-lapachone showed activity only against M. marinum. The most active substances for M. kansasii were the derivates 2, 3, 7, and 11, in which compound 2 (CMI = 0.96 μM) was the most active. For M. marinum, 2, 11, and 14 were the most active, while against M. abcessus the compound 3 was the only active. The results showed a wide and diversified resistance spectrum among the species studied, which could be related to the molecular structure and position of the substituting groups, indicating the potentiality of these molecules as antimicrobial prototypes., Colegio de Farmacéuticos de la Provincia de Buenos Aires

Published
2012

4. In vitro anti-mycobacterial activity of (E)-N'-(monosubstituted-benzylidene) isonicotinohydrazide derivatives against isoniazidresistant strains.

Author

Coelho, Tatiane S., Cantos, Jessica B., Bispo, Marcelle L. F., Gonçalves, Raoni S. B., Lima, Camilo H. S., Da Silva, Pedro E. A., and Souza, Marcus V. N.

Subjects
*LUNG diseases, *TUBERCULOSIS, *CHEST diseases, *MYCOBACTERIAL diseases, *ANTITUBERCULAR agents, *ISONICOTINIC acid
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. [ABSTRACT FROM AUTHOR]

Published
2012
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