Synthesis and activity study of phosphonamidate dipeptides as potential inhibitors of VanX

KW Yang, X Cheng, C Zhao, CC Liu, C Jia…

Index: Yang, Ke-Wu; Cheng, Xu; Zhao, Chuan; Liu, Cheng-Cheng; Jia, Chao; Feng, Lei; Xiao, Jian-Min; Zhou, Li-Sheng; Gao, Hui-Zhou; Yang, Xia; Zhai, Le Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 23 p. 7224 - 7227

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Citation Number: 4

Abstract

In an effort to develop inhibitors of VanX, the phosphonamidate analogs of d-Ala-d-Ala dipeptides, N-[(1-aminoethyl) hydroxyphosphinyl]-glycine (1a),-alanine (1b),-valine (1c),- leucine (1d) and-phenylalanine (1e) were synthesized, characterized and evaluated using recombinant VanX. The crystal structure of the intermediate 6d was obtained (Deposition number: CCDC 839134), and structural analysis revealed that it is orthorhombic with a ...