Parallel synthesis of a library of 1,4-naphthoquinones and automated screening of potential inhibitors of trypanothione reductase from Trypanosoma cruzi

Citation
L. Salmon-chemin et al., Parallel synthesis of a library of 1,4-naphthoquinones and automated screening of potential inhibitors of trypanothione reductase from Trypanosoma cruzi, BIOORG MED, 10(7), 2000, pp. 631-635
Citations number
12
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
7
Year of publication
2000
Pages
631 - 635
Database
ISI
SICI code
0960-894X(20000403)10:7<631:PSOALO>2.0.ZU;2-J
Abstract
Solid- and solution-phase parallel syntheses of 1,4-naphthoquinones (1,4-NQ ) are described. A library of 1360 amides was constructed from the combinat ion of 12 newly synthesised 1,4-NQ carboxylic acid and 120 amines, and was screened for inhibition of trypanothione reductase (TR) from Trypanosoma cr uzi. The most active hits from a primary screening were re-synthesised and confirmed. This approach proves that it is possible to design potent and hi ghly specific TcTR inhibitors deriving From menadione, juglone and plumbagi n. (C) 2000 Elsevier Science Ltd. All rights reserved.