Literature

Abstract

As an extension of research, we have investigated modification of left-hand side (LHS) of biphenyl analogues containing an acylsulfonamide moiety in the development of potent and selective human beta(3)-adrenergic receptor (AR) agonists. Result of structure-activity relationships (SAR) and cassette-dosing evaluation in dogs showed that the hydroxynorephedrine analogue 16 had an excellent balance of in vitro and in vivo potency with pharmacokinetic profiles. In addition, to facilitate structure-based drug design (SBDD), we also have performed a docking study of biphenyl analogues based on the X-ray structure of the beta(2)-adrenergic receptor.

DOI： 10.1016/j.bmcl.2009.06.083

Discovery of highly potent and selective biphenylacylsulfonamide-based β3-adrenergic receptor agonists and molecular modeling based on the solved X-ray structure of the β2-adrenergic receptor: Part 6

Bioorganic & Medicinal Chemistry Letters 2009.0

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, potent and selective human β3-adrenergic receptor agonist

Bioorganic & Medicinal Chemistry Letters 2005.0

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

Synthesis and Evaluation of Potent and Selective β3 Adrenergic Receptor Agonists Containing Acylsulfonamide, Sulfonylsulfonamide, and Sulfonylurea Carboxylic Acid Isosteres

Journal of Medicinal Chemistry 2002.0

Discovery of Highly Potent and Selective Biphenylacylsulfonamide-Based β3-Adrenergic Receptor Agonists and Evaluation of Physical Properties as Potential Overactive Bladder Therapies: Part 5