Bioorganic & Medicinal Chemistry 2013-03-01

Polyamino geranic derivatives as new chemosensitizers to combat antibiotic resistant gram-negative bacteria.

Jean Michel Brunel, Aurélie Lieutaud, Vincent Lome, Jean-Marie Pagès, Jean-Michel Bolla

Index: Bioorg. Med. Chem. 21(5) , 1174-9, (2013)

Full Text: HTML

Abstract

Benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate reagent (BOP) serves as an efficient and versatile coupling reagent for the design and synthesis of new polyamino geranic acid derivatives in moderate to good chemical yields varying from 47% to 83%. These compounds induced a significant decrease of antibiotic resistance in two Gram-negative bacterial MDR strains. Our data suggested that their mechanism of action is closely associated with the inhibition of the efflux pumps.Copyright © 2012 Elsevier Ltd. All rights reserved.