Title : Discovery of Novel Indazole Derivatives as Orally Available β3-Adrenergic Receptor Agonists Lacking Off-Target-Based Cardiovascular Side Effects.

Pub. Date : 2017 Apr 27

PMID : 28355078






1 Functional Relationships(s)
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1 We focused on the sulfonamide moiety of this scaffold, which resulted in the discovery of compound 15 as a highly potent beta3-AR agonist (EC50 = 18 nM) being inactive to beta1-, beta2-, and alpha1A-AR (beta1/beta3, beta2/beta3, and alpha1A/beta3 > 556-fold). Sulfonamides adrenoceptor beta 3 Rattus norvegicus