Discovery of potent and orally active MTP inhibitors as potential anti-obesity agents

Bioorg Med Chem Lett. 2006 Jun 1;16(11):3039-42. doi: 10.1016/j.bmcl.2006.02.058. Epub 2006 Mar 10.

Abstract

We have successfully identified a number of novel MTP inhibitors with single digit nanomolar potency. Analogues 10aq and 10dq demonstrated in vivo efficacy in a murine gut retention assay.

MeSH terms

  • Administration, Oral
  • Animals
  • Anti-Obesity Agents / administration & dosage
  • Anti-Obesity Agents / chemical synthesis*
  • Anti-Obesity Agents / chemistry
  • Anti-Obesity Agents / pharmacology*
  • Carrier Proteins / antagonists & inhibitors*
  • Carrier Proteins / metabolism
  • Mice
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Anti-Obesity Agents
  • Carrier Proteins
  • microsomal triglyceride transfer protein