Automated parallel synthesis of a tetrahydroisoquinolin-based library: Potential prolyl endopeptidase inhibitors

Citation
S. Vendeville et al., Automated parallel synthesis of a tetrahydroisoquinolin-based library: Potential prolyl endopeptidase inhibitors, BIOORG MED, 9(3), 1999, pp. 437-442
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
3
Year of publication
1999
Pages
437 - 442
Database
ISI
SICI code
0960-894X(19990208)9:3<437:APSOAT>2.0.ZU;2-B
Abstract
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.