Synthesis and antimicrobial activity of α-aminoboronic-containing peptidomimetics.
A library of 175 dipeptidomimetics and tripeptidomimetics containing an α-amino boronic acid or boronate has been synthesized, and the activity toward Mycobacterium tuberculosis, Candida albicans, Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli and Pseudomonas aeruginosa has been screened. Although there is no clear structure-activity relationship, several compounds exhibit promising activity against different pathogens.
Department of Chemistry, University of Tromsø, Tromsø, Norway.
Olga V
OV
Gozhina
John Sigurd
JS
Svendsen
Tore
T
Lejon
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001897:Boronic Acids / Q000138:chemical synthesis / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects; D004926:Escherichia coli / Q000187:drug effects; D056945:Hep G2 Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D018716:Molecular Mimicry; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D057786:Peptidomimetics / Q000138:chemical synthesis / Q000494:pharmacology*; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects; D013297:Streptococcus pyogenes / Q000187:drug effects; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D001897:Boronic Acids; D057786:Peptidomimetics
Matteson homologation; antimicrobials; α-amino boronate; α-amino boronic acid