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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Review Article

Towards the Development of Synthetic Antibiotics: Designs Inspired by Natural Antimicrobial Peptides

Author(s): Fazren Azmi, Mariusz Skwarczynski and Istvan Toth

Volume 23, Issue 41, 2016

Page: [4610 - 4624] Pages: 15

DOI: 10.2174/0929867323666160825162435

Price: $65

Abstract

Virtually every living organism produces gene-encoded antimicrobial peptides (AMPs) that provide an immediate defence against pathogen invasion. Many AMPs have been isolated and used as antibiotics that are effective against multidrug-resistant bacteria. Although encouraging, AMPs have such poor drug-like properties that their application for clinical use is restricted. In turn, this has diverted research to the development of synthetic molecules that retain the therapeutic efficacy of AMPs but are endowed with greater biological stability and safety profiles. Most of the synthetic molecules, either based on a peptidic or non-peptidic scaffold, have been designed to mimic the amphiphilic properties of native AMPs, which are widely believed to be the key determinant of their antibacterial activity. In this review, the structural, chemical and biophysical features that govern the biological activities of various synthetic designs are discussed extensively. Recent innovative approaches from the literature that exhibit novel concepts towards the development of new synthetic antibacterial agents, including the engineered delivery platform incorporated with AMP mimetics, are also emphasised.

Keywords: Antimicrobial peptides, synthetic mimics, antibacterial, amphiphilic properties, multidrug-resistant bacteria, peptide, polymer, peptidomimetics.


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