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Title: Membrane Active Phenylalanine Conjugated Lipophilic Norspermidine Derivatives with Selective Antibacterial Activity
Authors: Konai, Mohini M.
Ghosh, Chandradhish
Yarlagadda, Venkateswarlu
Samaddar, Sandip
Haldar, Jayanta
Keywords: Medicinal Chemistry
Helical Antimicrobial Peptides
De-Novo Design
Peptoid Mimics
Issue Date: 2014
Publisher: American Chemical Society
Citation: Konai, MM; Ghosh, C; Yarlagadda, V; Samaddar, S; Haldar, J, Membrane Active Phenylalanine Conjugated Lipophilic Norspermidine Derivatives with Selective Antibacterial Activity. Journal of Medicinal Chemistry 2014, 57 (22) 9409-9423,
Journal of Medicinal Chemistry
Abstract: Natural and synthetic membrane active antibacterial agents offer hope as potential solutions to the problem of bacterial resistance as the membrane-active nature imparts low propensity for the development of resistance. In this report norspermidine based antibacterial molecules were developed that displayed excellent antibacterial activity against various wild-type bacteria (Gram-positive and Gram-negative) and drug-resistant bacteria (methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus faecium, and beta-lactam-resistant Klebsiella pneumoniae). In a novel structureactivity relationship study it has been shown how incorporation of an aromatic amino acid drastically improves selective antibacterial activity. Additionally, the effect of stereochemistry on activity, toxicity, and plasma stability has also been studied. These rapidly bactericidal, membrane active antibacterial compounds do not trigger development of resistance in bacteria and hence bear immense potential as therapeutic agents to tackle multidrug resistant bacterial infections.
Description: Restricted Access
ISSN: 0022-2623
Appears in Collections:Research Papers (Jayanta Haldar)

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