Prodrugs of CL316243: a selective beta3-adrenergic receptor agonist for treating obesity and diabetes

Bioorg Med Chem Lett. 1999 Jul 19;9(14):1921-6. doi: 10.1016/s0960-894x(99)00316-9.

Abstract

CL316243 is a highly selective and potent beta3-adrenergic receptor agonist, and has been shown in rodent models to be an effective agent for treating obesity and Type II diabetes. To improve the oral absorption and pharmacokinetic profiles of CL316243, a number of prodrugs have been synthesized and evaluated. Several ester-type prodrugs show significant improvements in oral bioavailability in both rodent and primate models.

MeSH terms

  • Adrenergic beta-Agonists / chemistry
  • Adrenergic beta-Agonists / metabolism
  • Adrenergic beta-Agonists / pharmacology*
  • Animals
  • Biological Availability
  • Diabetes Mellitus, Experimental / drug therapy*
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Dioxoles / pharmacology*
  • Esters / chemistry
  • Esters / metabolism
  • Fatty Acids / blood
  • Half-Life
  • Haplorhini
  • Humans
  • Hydrolysis
  • Hypoglycemic Agents / pharmacology*
  • Mice
  • Obesity / drug therapy*
  • Prodrugs / chemistry
  • Prodrugs / metabolism
  • Prodrugs / pharmacology*
  • Rats

Substances

  • Adrenergic beta-Agonists
  • Dioxoles
  • Esters
  • Fatty Acids
  • Hypoglycemic Agents
  • Prodrugs
  • disodium (R,R)-5-(2-((2-(3-chlorophenyl)-2-hydroxyethyl)-amino)propyl)-1,3-benzodioxole-2,3-dicarboxylate