Bioorganic and Medicinal Chemistry Letters p. 2957 - 2961 (2002)
Update date:2022-08-05
Topics:
Steffan, Robert J.
Ashwell, Mark A.
Solvibile, William R.
Matelan, Edward
Largis, Elwood
Han, Stella
Tillet, Jeffery
Mulvey, Ruth
The synthesis and SAR of a series of human β3 adrenoreceptor agonists based on a template derived from a common pharmacophore coupled with 4-aminomethylpiperidine is described. Potent and selective agents were identified such as 26 that was in vitro active in CHO cells expressing human β3-AR (EC50=49 nM, IA=1.1), and in vivo active in a transgenic mouse model.
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