A disubstituted NAD(+) analogue is a nanomolar inhibitor of trypanosomal glyceraldehyde-3-phosphate dehydrogenase

Authors
Kennedy, KJ Bressi, JC Gelb, MH
Citation
Kj. Kennedy et al., A disubstituted NAD(+) analogue is a nanomolar inhibitor of trypanosomal glyceraldehyde-3-phosphate dehydrogenase, BIOORG MED, 11(2), 2001, pp. 95-98
Citations number
12
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
2
Year of publication
2001
Pages
95 - 98
Database
ISI
SICI code
0960-894X(20010122)11:2<95:ADNAIA>2.0.ZU;2-N
Abstract
N-6-Naphthalenemethyl-2'-methoxybenzamido-beta -NAD(+), a derivative of a l ow micromolar first-generation inhibitor of trypanosomal glyceraldehyde pho sphate dehydrogenase (GAPDH), was synthesized, taking advantage of methodol ogy for the selective phosphitylation of nucleosides. The compound was foun d to be a poor alternate cosubstrate for GAPDH, but an extremely potent inh ibitor. Although intended for use in crystallization trials, the analogue p resents possibilities for further drug design. (C) 2001 Elsevier Science Lt d. All rights reserved.