S. Vendeville et al., Automated parallel synthesis of a tetrahydroisoquinolin-based library: Potential prolyl endopeptidase inhibitors, BIOORG MED, 9(3), 1999, pp. 437-442
Solution-phase automated parallel synthesis of a Tie-based library is descr
ibed. This library comprising 2560 members, was obtained from the combinati
on of 80 carboxylic acids and 32 amines and was screened against Tc80 prote
ase, a parasitic prolyl endopeptidase secreted by Trypanosoma cruzi. Pyrrol
idine derivatives proved the most potent inhibitors with IC50 values found
in the low nanomolar range. (C) 1999 Elsevier Science Ltd. All rights reser
ved.