Phosphono- and Phosphinopeptides

In the past few years, intensive efforts have been made to create novel and original syn thetic oligomers. Many different modifications have been introduced to replace the labil peptide bond. Among the various positive developments in this field, the discovery c molecules with improved pharmacological properties compared to those of natural pep tides can be considered one of the most important. The study of the new conformationt features of these synthetic frameworks can supply additional information on the strut ture-activity relationships. 

In conclusion, research in the field of combinatorial synthetic oligomers for drug di covery is showing both continuous and beneficial progress, and new creative scaffolds wi undoubtedly be proposed in the near future. 

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Palacios, F., Alonso, C., and de los Santos, J. (2004) /i-Phosphono- and phosphinopeptides derived from /3-amino-phosphonic and phosphinic acids. Curr. Org. Chem. 8,1481-1496. 

In 1975, Marthell et al. introduced the term phosphonopeptides for peptide analogues in which an aminocarboxylic residue is replaced by an aminophosphonate at any position in the peptide chain [94]. There is an excellent review by P. Kafarski and B. Lejczak [95] devoted to the synthesis of phosphono- and phosphinopeptides. Here, only references connected with the synthesis of biologically active phosphonopeptides using aminophosphonates based on H-hosphonate diesters have been included. 

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