2. Academic Validation
  3. SAR and species/stereo-selective metabolism of the sorbitol dehydrogenase inhibitor, CP-470,711

SAR and species/stereo-selective metabolism of the sorbitol dehydrogenase inhibitor, CP-470,711

  • Bioorg Med Chem Lett. 2002 Jun 3;12(11):1477-80. doi: 10.1016/s0960-894x(02)00208-1.
Margaret Y Chu-Moyer 1,  William E Ballinger,  David A Beebe,  James B Coutcher,  Wesley W Day,  Jiancheng Li,  Peter J Oates,  R Matthew Weekly
Affiliations

Affiliation

  • 1 Cardiovascular and Metabolic Diseases, Pfizer Global Research and Development, Groton Laboratories MS8220-3095, Eastern Point Road, CT 06340, USA. margaret_y_chu-moyer@groton.pfizer.com
PMID: 12031323 DOI: 10.1016/s0960-894x(02)00208-1
Abstract

SAR studies on the stereoisomers of CP-470,711 suggested that in vivo epimerization was taking place in rats. Further metabolism studies revealed that no epimerization was occurring in dogs, and that no epimerization was expected in humans. A mechanism for the in vivo epimerization is proposed involving an oxidation-reduction pathway of the secondary benzylic alcohol, in contrast to an acid/base-promoted epimerization of the same center during chemical synthesis.

Figures
Products