This Article
Right arrow Full Text
Right arrow Full Text (PDF)
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Right arrowReprints and Permissions
Right arrow Copyright Information
Right arrow Books from ASM Press
Right arrow MicrobeWorld
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Maccari, R.
Right arrow Articles by Vigorita, M. G.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Maccari, R.
Right arrow Articles by Vigorita, M. G.

 Previous Article  |  Next Article 

Antimicrobial Agents and Chemotherapy, February 2002, p. 294-299, Vol. 46, No. 2
0066-4804/01/$04.00+0     DOI: 10.1128/AAC.46.2.294-299.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

In Vitro Antimycobacterial Activities of 2'-Monosubstituted Isonicotinohydrazides and Their Cyanoborane Adducts

Rosanna Maccari,* Rosaria Ottanà, Francesca Monforte, and Maria Gabriella Vigorita

Dipartimento Farmaco-Chimico, Facoltà di Farmacia, Università di Messina, 98168 Messina, Italy

Received 11 June 2001/ Returned for modification 30 July 2001/ Accepted 22 October 2001

As a result of our search for new isoniazid derivatives with extended spectra of activity, we evaluated the in vitro antimycobacterial activities of isonicotinohydrazides (compounds 2) and their cyanoborane adducts (compounds 3), both obtained by the reaction of isonicotinoylhydrazones (compounds 1) with sodium cyanoborohydride. Most of the tested compounds displayed moderate to high activity against Mycobacterium tuberculosis H37Rv, with MICs ranging from 0.2 to 12.5 µg/ml. In particular, some hydrazides showed activity similar to that of rifampin (MIC = 0.2 µg/ml) and rather low cytotoxicity, so that they were generally shown to possess high safety indices. In contrast, the coordination to a cyanoborane (BH2CN) group (compounds 3) in general brought about a decrease in antimycobacterial activity, while cytotoxicity increased. Interestingly, selected compounds 1 to 3, mostly hydrazides (compounds 2), were effective in killing M. tuberculosis growing within macrophages at concentrations in culture medium which were much lower than the corresponding MICs. These compounds also displayed good activity against drug-resistant M. tuberculosis strains.

* Corresponding author. Mailing address: Dipartimento Farmaco-chimico, Facoltà di Farmacia, Università di Messina, Vl. SS. Annunziata, 98168 Messina, Italy. Phone: 01139 90 6766406. Fax: 01139 90 355613. E-mail: rmaccari{at}pharma.unime.it.

Antimicrobial Agents and Chemotherapy, February 2002, p. 294-299, Vol. 46, No. 2
0066-4804/01/$04.00+0     DOI: 10.1128/AAC.46.2.294-299.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.



This article has been cited by other articles:

  • Hearn, M. J., Cynamon, M. H. (2004). Design and synthesis of antituberculars: preparation and evaluation against Mycobacterium tuberculosis of an isoniazid Schiff base. J Antimicrob Chemother 53: 185-191 [Abstract] [Full Text]  


Copyright © 2009 by the American Society for Microbiology.   For an alternate route to Journals.ASM.org, visit: http://intl-journals.asm.org | More Info»