creators_name: Lohan, Sandeep
creators_name: Cameotra, Swaranjit Singh
creators_name: Bisht, Gopal Singh
type: article
datestamp: 2015-02-09 11:27:38
lastmod: 2015-02-09 11:27:38
metadata_visibility: show
title: Antibacterial evaluation of structurally amphipathic, membrane active small cationic peptidomimetics: synthesized by incorporating 3-amino benzoic acid as peptidomimetic element.
ispublished: pub
keywords: 3-Amino benzoic acid; Antibacterial peptidomimetics; Antibiotic resistance; Plasma stability
abstract: A new series of small cationic peptidomimetics were synthesized by incorporating 3-amino benzoic acid (3-ABA) in a small structural framework with the objective to mimic essential properties of natural antimicrobial peptides (AMPs). The new design approach resulted into improvement of activity and selectivity in comparison to linear peptides and allowed us to better understand the influence of structural amphipathicity on biological activity. Lead peptidomimetics displayed antibacterial activities against resistant pathogens (MRSA & MRSE). A calcein dye leakage experiment revealed a membranolytic effect of 4g and 4l which was further confirmed by fluorescence microscopy. In addition, proteolytic stability and no sign of resistance development against Staphylococcus aureus and MRSA demonstrate their potential for further development as novel antimicrobial therapeutics.
date: 2014-08-18
date_type: published
publication: European journal of medicinal chemistry
volume: 83
publisher: Paris : Editions Scientifiques Elsevier
pagerange: 102-15
refereed: TRUE
issn: 1768-3254
official_url: http://www.sciencedirect.com/science/article/pii/S022352341400542X
citation:   Lohan, Sandeep and Cameotra, Swaranjit Singh and Bisht, Gopal Singh  (2014) Antibacterial evaluation of structurally amphipathic, membrane active small cationic peptidomimetics: synthesized by incorporating 3-amino benzoic acid as peptidomimetic element.  European journal of medicinal chemistry, 83.  pp. 102-15.  ISSN 1768-3254