Dipeptide vinyl sultams: Synthesis via the Wittig–Horner reaction and activity against papain, falcipain-2 and Plasmodium falciparum

C Valente, RC Guedes, R Moreira, J Iley, J Gut…

文献索引：Valente, Claudia; Guedes, Rita C.; Moreira, Rui; Iley, Jim; Gut, Jiri; Rosenthal, Philip J. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 15 p. 4115 - 4119

全文：HTML全文

被引用次数: 42

摘要

The synthesis of phosphonate derivatives of N-phenyl-and N-benzyl-γ-and δ-sultams, and their application in the Wittig-Horner reaction with N-Boc-l-phenylalanine aldehyde to afford E-and Z-isomers, are described. These compounds were further processed to provide five dipeptide vinyl sultams, which were found to be inactive against papain at concentrations up to 50μM. In contrast, vinyl sultams demonstrated weak activity against recombinant ...