title: Synthesis and preliminary antibacterial evaluation of simplified thiomarinol analogs.
abstract: A series of simplified thiomarinol derivatives was prepared by way of catalytic enantioselective inverse electron demand hetero [4+2] cycloaddition/allylboration tandem reaction. As a preliminary evaluation, these analogs were tested for antimicrobial activity using a standard disk diffusion assay. Whereas amide analogs were less active, the simple ester analogs 3 and 4 were demonstrated to be more active than thiomarinol H.
authors.affiliation: Department of Chemistry, University of Alberta, Edmonton, AB, Canada T6G 2G2.
authors.forename: Olivier
authors.initials: O
authors.lastname: Marion
authors.forename: Xuri
authors.initials: X
authors.lastname: Gao
authors.forename: Sandra
authors.initials: S
authors.lastname: Marcus
authors.forename: Dennis G
authors.initials: DG
authors.lastname: Hall
mesh_terms: D000604:Amino Acyl-tRNA Synthetases / Q000037:antagonists & inhibitors / Q000378:metabolism; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D003500:Cyclization; D052978:Disk Diffusion Antimicrobial Tests; D016712:Mupirocin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; C085617:thiomarinol; D016712:Mupirocin; D000604:Amino Acyl-tRNA Synthetases