Pharmacophoric mapping based on 3D-QSAR studies is performed on sixteen cyclic ureidobenzenesulfonamides for their beta(3)-adrenergic receptor agonistic activity. The best 3D-QSAR model (with r(2)=0.877) which described the properties and distributions of 5-biophoric and 2-secondary biophoric sites, showed a good correlation between the observed and predicted activity both in training and test.

01 Mar 1999·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Human β3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides

Q4 · MEDICINE

Article

Author: MacIntyre, D. Euan ; Hom, Gary J. ; Strader, Catherine D. ; Perkins, Leroy ; Ok, Hyun O. ; Cascieri, Margaret A. ; Wyvratt, Matthew J. ; Deng, Liping ; Parmee, Emma R. ; Colandrea, Vincent J. ; Miller, Randall R. ; Candelore, Mari R. ; Tota, Laurie ; Feeney, William P. ; Stearns, Ralph A. ; Naylor, Elizabeth M. ; Weber, Ann E. ; Fisher, Michael H. ; Forrest, Michael J.

Human beta3 adrenergic receptor agonists containing 5-membered ring ureas were shown to be potent partial agonists with excellent selectivity over beta1 and beta2 binding. L-760,087 (4a) and L-764,646 (5a) (beta3 EC50 = 18 and 14 nM, respectively) stimulate lipolysis in rhesus monkeys (ED50 = 0.2 and 0.1 mg/kg, respectively) with minimal effects on heart rate. Oral absorption in dogs is improved over other urea analogs.

01 Mar 1999·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Human β3 andrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides

Q4 · MEDICINE

Article

Author: Tota, Laurie ; Deng, Liping ; Naylor, Elizabeth M. ; Cascieri, Margaret A. ; Wyvratt, Matthew J. ; Parmee, Emma R. ; Brockunier, Linda ; Candelore, Mari R. ; Wang, Pei-Ran ; Hom, Gary J. ; Strader, Catherine D. ; Feeney, William P. ; Forrest, Michael J. ; Colwell, Lawrence F. Jr. ; Weber, Ann E. ; MacIntyre, D. Euan ; Perkins, Leroy ; Fisher, Michael H. ; Colandrea, Vincent J.

The cyclopentylpropylimidazolidinone L-766,892 is a potent beta3 AR agonist (EC50 5.7 nM, 64% activation) with 420- and 130-fold selectivity over binding to the beta1 and beta2 ARs, respectively. In anesthetized rhesus monkeys, L-766,892 elicited dose-dependent hyperglycerolemia (ED50 0.1 mg/kg) with minimal effects on heart rate.

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Indication	Highest Phase	Country/Location	Organization	Date
Obesity	Preclinical	United States	Merck & Co., Inc.	30 Apr 1999

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