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Antimicrobial Activity of Short, Synthetic Cationic Lipopeptides
Author(s) -
Laverty Garry,
McLaughlin Martin,
Shaw Christopher,
Gorman Sean P.,
Gilmore Brendan F.
Publication year - 2010
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2010.00973.x
Subject(s) - antimicrobial , cationic polymerization , tetrapeptide , chemistry , microbiology and biotechnology , antibiotic resistance , multiple drug resistance , bacteria , antibiotics , combinatorial chemistry , biofilm , biology , biochemistry , peptide , organic chemistry , genetics
The increasing emergence of multidrug‐resistant micro‐organisms presents one of the greatest challenges in the clinical management of infectious diseases. Therefore, novel antimicrobial agents are urgently required to address this issue. In this report, we describe the solid phase synthesis, characterization, microbiological and toxicological evaluation of a library of ultrashort cationic antimicrobial lipopeptides based on the previously described tetrapeptide amide H‐Orn‐Orn‐Trp‐Trp‐NH 2 conjugated with saturated fatty acids which have inherent antimicrobial activity. The microbiological activity of these ultrashort cationic lipopeptides, which exhibit excellent, broad‐spectrum antimicrobial activity against a number of clinically important pathogenic bacteria and fungi, including multidrug resistant micro‐organisms in both planktonic and sessile (biofilm) cultures is reported.