2. Academic Validation
  3. A disubstituted NAD+ analogue is a nanomolar inhibitor of trypanosomal glyceraldehyde-3-phosphate dehydrogenase

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

  • Bioorg Med Chem Lett. 2001 Jan 22;11(2):95-8. doi: 10.1016/s0960-894x(00)00608-9.
K J Kennedy 1,  J C Bressi,  M H Gelb
Affiliations

Affiliation

  • 1 Department of Chemistry, University of Washington, Seattle 98195, USA.
PMID: 11206479 DOI: 10.1016/s0960-894x(00)00608-9
Abstract

N6-Naphthalenemethyl-2'-methoxybenzamido-beta-NAD+, a derivative of a low micromolar first-generation inhibitor of trypanosomal glyceraldehyde phosphate dehydrogenase (GAPDH), was synthesized, taking advantage of methodology for the selective phosphitylation of nucleosides. The compound was found to be a poor alternate cosubstrate for GAPDH, but an extremely potent inhibitor. Although intended for use in crystallization trials, the analogue presents possibilities for further drug design.

Figures