Frank Ratcliffe Atherton

TL;DR: In this paper, a method for large-scale synthesis of the potent antibacterial agent L-Ala-L -Ala(P) (1, Alafosfalin) is described.

TL;DR: Certain phosphonopeptides, of which L-alanyl-‘L’-l-aminoethylphosphonic acid (alaphosphin) is typical, inhibit the growth of various important pathogenic bacteria in vitro and in infected animals.

TL;DR: The novel antibacterial peptide mimetic alaphosphin (l-alanyl-l-1-aminoethylphosphonic acid) selectively inhibited peptidoglycan biosynthesis in both gram-negative and gram-positive bacteria.

TL;DR: The in vitro antibacterial activities of representative phosphonodi- to phosphonohexapeptides were investigated and the phosphonopeptide series consisting of various l and d residues of natural amino acids combined with 1-aminoalkyl (and aryl-alkyl-) phosphonic acid residues had the most interesting antibacterial properties.

TL;DR: Alaphosphin was equally effective against penicillin-susceptible and -resistant strains and showed no cross-resistance with known antibiotics, and good synergy and increased bactericidal activity were demonstrated with combinations of alaph phosphin and d-cycloserine or β-lactam antibiotics.