Synthesis and evaluation of galactofuranosyl N,N-dialkyl sulfenamides and sulfonamides as antimycobacterial agents
| Autor: | Robin J. Thomson, David J. Owen, Mark von Itzstein, Ross L. Coppel, Andrew Chong, Regan David Hartnell, Paul D. Madge, Christopher Davis |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Tuberculosis
Mycobacterium smegmatis Clinical Biochemistry Pharmaceutical Science Microbial Sensitivity Tests Sulfamerazine Biochemistry Microbiology Mycobacterium tuberculosis Structure-Activity Relationship Drug Discovery medicine Molecular Biology Pathogen Antibacterial agent Sulfonamides biology Chemistry Organic Chemistry Sulfonamide (medicine) Biological activity biology.organism_classification medicine.disease Anti-Bacterial Agents Molecular Medicine medicine.drug Mycobacterium |
| Zdroj: | Monash University |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2007.01.068 |
| Popis: | The recent emergence of clinically oppressive superbugs, some with resistance to nearly all frontline drug therapies, has challenged our ability to combat such infectious organisms as Mycobacterium tuberculosis, the causative agent of tuberculosis (TB). Our medicinal chemistry program targeting this pathogen has identified several potent galactofuranose-based in vitro inhibitors of mycobacterial growth. The most potent compound, the Galf N,N-didecyl sulfenamide 8d, displayed anti-mycobacterial activity (MIC) of 1 microg/mL in a cell based assay against a representative strain of Mycobacterium smegmatis. |
| Databáze: | OpenAIRE |
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