Prodrugs of CL316243: a selective β3-adrenergic receptor agonist for treating obesity and diabetes

Abstract CL316243 is a highly selective and potent β 3 -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.