Synthesis of phosphinic alanyl-proline surrogates Alaψ(PO2R-CH)Pro as potential inhibitors of the human cyclophilin hCyp-18

Pseudopeptides containing the phosphinic analogue of the alanyl-proline motif Alaψ(PO2R-CH)Pro, were synthesized via three- (R=H) and four-step (R=CH3) procedures. The mixtures of diastereomers were evaluated as inhibitors of the human cyclophilin hCyp-18, an important peptidyl-prolyl isomerase.