New oxadiazolidinedione derivatives as potent and selective human beta3 agonists

Bioorganic & Medicinal Chemistry Letters
B HuJ Tillett

Abstract

As part of our investigation into the development of potent and selective human beta3 agonists, a series of thiazolidinedione analogues was prepared and evaluated for their biological activity on the human beta3-adrenergic receptor. The oxadiazolidinedione derivative 17 was found to be the most potent and selective compound in this study, with an EC50 value of 0.02 microM at the beta3 receptor, 259-fold selectivity over the beta1 receptor, and 745-fold selectivity over the beta2 receptor.

References

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Citations

Dec 21, 2010·Medicinal Chemistry Research : an International Journal for Rapid Communications on Design and Mechanisms of Action of Biologically Active Agents·P Senthil Kumar, Prasad V Bharatam
Sep 8, 2001·Drug Discovery Today·S Langston, D Barlocco
Oct 25, 2008·Journal of Medicinal Chemistry·Toni KlineSamuel I Miller

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