Amino acids

The synthesis and biological testing of bacilysin analogues

K Robertson, CD Murphy, F Paradisi

Index: Robertson, Keith; Murphy, Cormac D.; Paradisi, Francesca Amino Acids, 2013 , vol. 45, # 5 p. 1157 - 1168

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Abstract

Abstract A series of compounds based on the structure of bacilysin were synthesised and tested for antibacterial activity. The key steps in the syntheses are the coupling of an iodide to a diketopiperazine (DKP) and mono-lactim ether scaffold, respectively. The diastereoselectivity of the coupling reactions was dependant on the scaffold, with selectivity for DKP of about 4: 1 and mono-lactim ether exceeding 98: 2. Subsequent elaboration of ...