Application of the Suzuki-Miyaura cross-coupling to increase antimicrobial potency generates promising novel antibacterials.
Antimicrobial peptides have been recognized as a novel class of antibiotics, and several candidates are currently in clinical trials. In this work, a tripeptide derivative containing 4-iodo phenylalanine has been derivatized through the Suzuki-Miyaura cross-coupling. This has enabled the rapid and efficient synthesis of an array of tripeptide derivatives encompassing novel biaryl moieties. The peptide derivatives show high activity against Gram-positive bacteria.
Haug
Bengt Erik
BE
Department of Chemistry, University of Tromsø, N-9037 Tromsø, Norway. bengt-erik.haug@farm.uib.no
Stensen
Wenche
W
Svendsen
John S
JS
D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D020013:Calcium Signaling; D004268:DNA-Binding Proteins / Q000037:antagonists & inhibitors; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D018408:Patch-Clamp Techniques; D010599:Pharmacokinetics; D011485:Protein Binding; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors; D015534:Trans-Activators / Q000037:antagonists & inhibitors; D000071230:Transcriptional Regulator ERG
D000900:Anti-Bacterial Agents; D004268:DNA-Binding Proteins; C072312:ERG protein, human; C103263:MCHR1 protein, human; D017481:Receptors, Somatostatin; D015534:Trans-Activators; D000071230:Transcriptional Regulator ERG