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ID: ALA1131931
Journal: Bioorg Med Chem Lett
Title: Automated parallel synthesis of a tetrahydroisoquinolin-based library: potential prolyl endopeptidase inhibitors.
Authors: Vendeville S, Bourel L, Davioud-Charvet E, Grellier P, Deprez B, Sergheraert C.
Abstract: Solution-phase automated parallel synthesis of a Tic-based library is described. This library comprising 2560 members, was obtained from the combination of 80 carboxylic acids and 32 amines and was screened against Tc80 protease, a parasitic prolyl endopeptidase secreted by Trypanosoma cruzi. Pyrrolidine derivatives proved the most potent inhibitors with IC50 values found in the low nanomolar range.
CiteXplore: 10091698