Helical peptide–polyamine and –polyether conjugates as synthetic ionophores

Publication date: Available online 24 October 2015
Source:Bioorganic & Medicinal Chemistry
Author(s): Monica Benincasa, Marco Francescon, Massimo Fregonese, Renato Gennaro, Paolo Pengo, Paola Rossi, Paolo Scrimin, Paolo Tecilla
Two new synthetic ionophores in which the hydrophobic portion is represented by a short helical Aib-peptide (Aib = α-amino-isobutyric acid) and the hydrophilic one is a poly-amino (1a) or a polyether (1b) chain have been prepared. The two conjugates show a high ionophoric activity in phospholipid membranes being able to efficiently dissipate a pH gradient and, in the case of 1b, to transport Na⁺ across the membrane. Bioactivity evaluation of the two conjugates shows that 1a has a moderate antimicrobial activity against a broad spectrum of microorganisms and it is able to permeabilize the inner and the outer membrane of E. coli cells.

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