title: Development of novel membrane active lipidated peptidomimetics active against drug resistant clinical isolates.
creator: Lohan, Sandeep
creator: Kalanta, Arneesh
creator: Sonkusre, Praveen
creator: Cameotra, Swaranjit Singh
creator: Bisht, Gopal Singh
description: A new series of small cationic lipidated peptidomimetics have been synthesized and found to be highly active against several susceptible as well as drug resistant clinical isolates of bacteria and fungi. All lipidated peptidomimetics do not cause significant lysis of human erythrocytes (HC50>200μg/mL). Calcein dye leakage experiment revealed membranolytic effect of LPEP08 which was further confirmed by scanning electron microscopy (SEM). The involvement of intracellular targets as an alternate mode of action was precluded by DNA retardation assay. Additionally, LPEP08 exhibit high proteolytic stability and dose not elicit resistance against drug resistant clinical isolate of Staphylococcusaureus, even after 16 rounds of passaging. These results demonstrate the potential of lipidated peptidomimetics as biocompatible anti-infective therapeutics.
publisher: Oxford : Elsevier Science
date: 2014-09-01
type: Article
type: PeerReviewed
relation: http://www.sciencedirect.com/science/article/pii/S0968089614005574
identifier:   Lohan, Sandeep and Kalanta, Arneesh and Sonkusre, Praveen and Cameotra, Swaranjit Singh and Bisht, Gopal Singh  (2014) Development of novel membrane active lipidated peptidomimetics active against drug resistant clinical isolates.  Bioorganic & medicinal chemistry, 22 (17).  pp. 4544-52.  ISSN 1464-3391     
relation: http://crdd.osdd.net/open/1573/