Non hemolytic short peptidomimetics as a new class of potent and broad-spectrum antimicrobial agents

Bioorg Med Chem Lett. 2013 Aug 15;23(16):4633-6. doi: 10.1016/j.bmcl.2013.06.016. Epub 2013 Jun 14.

Abstract

Since the bacterial resistance to antibiotics is increasing rapidly, numerous studies have contributed to the design and synthesis of potent synthetic mimics of antimicrobial peptides (AMPs). In an attempt to find the pharmacophore of short antimicrobial peptidomimetics through systematic tuning of hydrophobic and hydrophilic patterns, we have identified a set of short histidine-derived antimicrobial peptides (SAMPs) with potent and broad-spectrum activity. A combination of high antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA), without hemolytic activity and proteolytic stability makes these molecules promising candidates for novel antimicrobial therapeutics.

Keywords: Methicillin-resistance Staphylococcus aureus; Proteolytic stability; Short antimicrobial peptidomimetics.

Publication types

  • Research Support, N.I.H., Intramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology*
  • Hemolysis
  • Methicillin-Resistant Staphylococcus aureus / drug effects*
  • Microbial Sensitivity Tests
  • Peptidomimetics*
  • Protein Stability

Substances

  • Anti-Infective Agents
  • Peptidomimetics