Amphipathic Barbiturates as Mimics of Antimicrobial Peptides and the Marine Natural Products Eusynstyelamides with Activity against Multi-resistant Clinical Isolates
Marianne H. Paulsen, Magnus Engqvist, Dominik Ausbacher, Trude Anderssen, Manuel K. Langer, Tor Haug, Glenn R. Morello, Laura E. Liikanen, Hans‐Matti Blencke, Johan Isaksson, Eric Juskewitz, Annette Bayer, Morten B. Strøm
Abstract
using a neutropenic peritonitis model. Mode of action studies showed a strong membrane disrupting effect and was supported by nuclear magnetic resonance and molecular dynamics simulations. The results express how the pharmacophore model of small AMPs and the structure of the marine eusynstyelamides can be used to design highly potent lead peptidomimetics against multi-resistant bacteria.
Topics & Concepts
PharmacophoreChemistryAntimicrobialBacteriaKlebsiella pneumoniaeAmphiphileCombinatorial chemistryEscherichia coliMicrobiologyStereochemistryBiochemistryOrganic chemistryBiologyCopolymerPolymerGeneticsGeneAntimicrobial Peptides and ActivitiesChemical Synthesis and AnalysisMicrobial Natural Products and Biosynthesis