title: Synthesis and evaluation of galactofuranosyl N,N-dialkyl sulfenamides and sulfonamides as antimycobacterial agents.
abstract: 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.
authors.affiliation: Institute for Glycomics, Griffith University (Gold Coast Campus), PMB 50 Gold Coast Mail Centre, Queensland 9726, Australia.
authors.forename: David J
authors.initials: DJ
authors.lastname: Owen
authors.forename: Chris B
authors.initials: CB
authors.lastname: Davis
authors.forename: Regan D
authors.initials: RD
authors.lastname: Hartnell
authors.forename: Paul D
authors.initials: PD
authors.lastname: Madge
authors.forename: Robin J
authors.initials: RJ
authors.lastname: Thomson
authors.forename: Andrew K J
authors.initials: AK
authors.lastname: Chong
authors.forename: Ross L
authors.initials: RL
authors.lastname: Coppel
authors.forename: Mark
authors.initials: M
authors.lastname: von Itzstein
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D020102:Mycobacterium smegmatis / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013416:Sulfamerazine / Q000138:chemical synthesis* / Q000494:pharmacology; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D013449:Sulfonamides; C471392:sulfenamide; D013416:Sulfamerazine