Literature

Abstract

Identification and SAR study of novel series of beta(3)-AR agonists with benzoic acid are described. Conversion of ether linkage position of phenoxybenzoic acid derivative 2b led to compound 7b with moderate beta(3)-AR activity. Further modification in right, center and left parts of compound 7b was investigated to improve the beta(3)-AR potency and selectivity. Compounds 7g and 7k, with the bulky aliphatic-substituted group at 2-position of benzoic acid moiety, were identified as potent and selective beta(3)-AR agonists. In addition, in vivo efficacy of compounds 7g and 7k was exhibited on dog OAB model.

DOI： 10.1016/j.bmcl.2008.08.009

Discovery of novel series of benzoic acid derivatives containing biphenyl ether moiety as potent and selective human β3-adrenergic receptor agonists: Part IV

Bioorganic & Medicinal Chemistry Letters 2008.0

Discovery of a Novel Series of Biphenyl Benzoic Acid Derivatives as Potent and Selective Human β3-Adrenergic Receptor Agonists with Good Oral Bioavailability. Part I

Journal of Medicinal Chemistry 2008.0

Discovery of a Novel Series of Biphenyl Benzoic Acid Derivatives as Highly Potent and Selective Human β3 Adrenergic Receptor Agonists with Good Oral Bioavailability. Part II

Journal of Medicinal Chemistry 2008.0

Discovery of a Novel Series of Benzoic Acid Derivatives as Potent and Selective Human β3Adrenergic Receptor Agonists with Good Oral Bioavailability. 3. Phenylethanolaminotetraline (PEAT) Skeleton Containing Biphenyl or Biphenyl Ether Moiety

Journal of Medicinal Chemistry 2008.0

Synthesis and evaluation of novel phenoxypropanolamine derivatives containing acetanilides as potent and selective β3-adrenergic receptor agonists

Bioorganic & Medicinal Chemistry 2009.0

Discovery of a novel, potent and selective human β3-adrenergic receptor agonist