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Title: Aryl-alkyl-lysines: Membrane-Active Small Molecules Active against Murine Model of Burn Infection
Authors: Ghosh, Chandradhish
Manjunath, Goutham B.
Konai, Mohini M.
Uppu, Divakara S. S. M.
Paramanandham, Krishnamoorthy
Shome, Bibek R.
Ravikumar, Raju
Haldar, Jayanta
Keywords: Pharmacology & Pharmacy
Infectious Diseases
antimicrobial peptides
antimicrobial resistance
burn infection
Combat Bacterial-Resistance
De-Novo Design
Antimicrobial Peptides
Persister Cells
Antibacterial Agents
Issue Date: 2016
Publisher: American Chemical Society
Citation: Ghosh, C.; Manjunath, G. B.; Konai, M. M.; Uppu, Dssm; Paramanandham, K.; Shome, B. R.; Ravikumar, R.; Haldar, J., Aryl-alkyl-lysines: Membrane-Active Small Molecules Active against Murine Model of Burn Infection. Acs Infectious Diseases 2016, 2 (2), 111-122
ACS Infectious Diseases
Abstract: Infections caused by drug-resistant Gramnegative pathogens continue to be significant contributors to human morbidity. The recent advent of New Delhi metallo-beta-lactamase-1 (blaNDM-1) producing pathogens, against which few drugs remain active, has aggravated the problem even further. This paper shows that aryl-alkyl-lysines, membrane active small molecules, are effective in treating infections caused by Gram-negative pathogens. One of the compounds of the study was effective in killing planktonic cells as well as dispersing biofilms of Gram-negative pathogens. The compound was extremely effective in disrupting preformed biofilms and did not select resistant bacteria in multiple passages. The compound retained activity in different physiological conditions and did not induce any toxic effect in female Balb/c mice until concentrations of 17.5 mg/kg. In a murine model of Acinetobacter baumannii burn infection, the compound was able to bring the bacterial burden down significantly upon topical application for 7 days.
Description: Restricted Access
ISSN: 2373-8227
Appears in Collections:Research Papers (Jayanta Haldar)

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