title: Click-based synthesis of bromotyrosine alkaloid analogs as potential anti-biofilm leads for SAR studies.
abstract: A library of triazole-based analogs of bromotyramine alkaloids such as verongamines, hemibastadins, pseudoceramine D and clavatidine E was designed in order to identify promising leads that may help in the control of bacterial biofilms. Twenty-three compounds were screened for their biofilm inhibitory activity against three strains of Gram-negative bacteria. SAR studies revealed that hemibastadins analogs were the most active compounds which act as inhibitors of biofilm development (EC50 8.8-29μM) without effect on bacterial growth even at high concentrations (100μM).
authors.affiliation: Université de Toulon, MAPIEM, EA 4323, 83957 La Garde, France.
authors.forename: S
authors.initials: S
authors.lastname: Andjouh
authors.affiliation: Université de Toulon, MAPIEM, EA 4323, 83957 La Garde, France. Electronic address: blache@univ-tln.fr.
authors.forename: Y
authors.initials: Y
authors.lastname: Blache
mesh_terms: D000470:Alkaloids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D018441:Biofilms / Q000187:drug effects; D057930:Click Chemistry; D006090:Gram-Negative Bacteria / Q000187:drug effects / Q000502:physiology; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D014443:Tyrosine / Q000031:analogs & derivatives* / Q000737:chemistry
chemical_list: D000470:Alkaloids; D000900:Anti-Bacterial Agents; D014230:Triazoles; C475724:bromotyrosine; D014443:Tyrosine
keywords: 1,2,3-Triazole; Biofilm; Bromotyrosine alkaloïds; Click chemistry