α-Aminoalkylphosphonates as a tool in experimental optimisation of P1 side chain shape of potential inhibitors in S1 pocket of leucine-and neutral aminopeptidases

…, J Grembecka, M Pawełczak, P Kafarski

Index: Drag, Marcin; Grembecka, Jolanta; Pawelczak, Malgorzata; Kafarski, Pawel European Journal of Medicinal Chemistry, 2005 , vol. 40, # 8 p. 764 - 771

Full Text: HTML

Citation Number: 50

Abstract

The synthesis and biological activity studies of the series of structurally different α- aminoalkylphosphonates were performed in order to optimise the shape of the side chain of the potential inhibitors in S1 pocket of leucine aminopeptidase [EC 3.4. 11.1]. Analysis of a series of compounds with aromatic, aliphatic and alicyclic P1 side chains enabled to find out the structural features, optimal for that fragment of inhibitors of LAP. The most active ...