Anti-mycobacterial activity of a bis-sulfonamide

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Title Anti-mycobacterial activity of a bis-sulfonamide
Author Wilkinson, Brendan Luke; Bornaghi, Laurent; Wright, Anthony D.; Houston, Todd Ashley; Poulsen, Sally-Ann
Journal Name Bioorganic & Medicinal Chemistry Letters
Year Published 2007
Place of publication United Kingdom
Publisher Pergamon Press
Abstract Since the introduction of prontosil over 70 years ago, sulfa drugs have been widely used to treat a broad spectrum of infectious microorganisms. The bioactive component of prontosil, sulfanilamide (1), inhibits 6-hydroxymethyl-7,8-dihydropteroate synthase (DHPS) selectively limiting folate synthesis in prokaryotes and lower eukaryotes thus disrupting the integrity of their DNA synthesis.1 The evolution of drug resistance in infectious microorganisms underpins an immense and ongoing need for new therapies to treat infectious diseases. The identification of new and novel chemical entities with activity against cells infected with the microorganism is a crucial component of this anti-infective drug development pathway.2 Although sulfonamides are not specifically incorporated into current tuberculosis treatment, many sulfur-3,4, sulfonyl-4,5,6, and sulfonamide-containing7,8 compounds are active against mycobacteria. This prompted us to screen our growing library of triazole-based sulfonamides (e.g.-2) for antimycobacterial activity. Herein we report identification of a novel bis-sulfonamide with antimicrobial activity against Mycobacterium smegmatis that is relatively inert toward common bacterial and fungal strains.
Peer Reviewed Yes
Published Yes
Publisher URI http://www.sciencedirect.com/science/journal/0960894X
Alternative URI http://dx.doi.org/10.1016/j.bmcl.2006.11.079
Volume 17
Page from 1355
Page to 1357
ISSN 0960-894X
Date Accessioned 2008-01-22
Language en_AU
Research Centre Eskitis Institute for Drug Discovery; Institute for Glycomics
Faculty Faculty of Science, Environment, Engineering and Technology
Subject PRE2009-Biological and Medical Chemistry
URI http://hdl.handle.net/10072/17944
Publication Type Journal Articles (Refereed Article)
Publication Type Code c1

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