Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Robert F. Day"'
Autor:
Margaret S. Landis, Robert F. Day, Joseph DiBrino, David A. Griffith, Robert L. Dow, Rebecca E. O’Connor, Philip A. Carpino, Paul DaSilva-Jardine, Shawn C Black, John R. Hadcock, Philip A. Iredale, Dennis O. Scott
Publikováno v:
Journal of Medicinal Chemistry. 52:234-237
We report the structure-activity relationships, design, and synthesis of the novel cannabinoid type 1 (CB1) receptor antagonist 3a (CP-945,598). Compound 3a showed subnanomolar potency at human CB1 receptors in binding (Ki = 0.7 nM) and functional as
Autor:
Oicheng Ng, Thomas A. Brown, Robert F. Day, Amy Brault, Robert L. Rosati, Bruce Allen Lefker, Pia Perry, Bihong Lu, Thomas A. Owen, Michael P. Zawistoski, Richard Chesworth, Tessa A. Castleberry, Kimberly O. Cameron, Lydia C. Pan, David D. Thompson, Paul DaSilva-Jardine, F.Michael Mangano, Stacy Colella, Donna N. Petersen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:2729-2733
Two series of 6-hydroxy and 7-hydroxy tetrahydroisoquinolines were prepared. Evaluating a range of C-1, C-4, and N-substituents led to the discovery of ER alpha and ER beta selective analogs.
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 39(12)
1-(8-(2-Chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl)-4-(ethylamino)piperidine-4-carboxamide (CP-945,598) is an orally active antagonist of the cannabinoid CB-1 receptor that progressed into phase 3 human clinical trials for the treatment of obesit
Autor:
Tristan S. Maurer, Kelly A. Martin, Robert F. Day, Jennifer Lafontaine, Diane M. Hargrove, John R. Hadcock, David A. Tess, Nancy A. Nardone, Paul DaSilva-Jardine, Joe Dibrino, Michael C. Linhares
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(18)
A novel series of heterocycle-based analogs were prepared and evaluated for their in vitro and in vivo biological activity as human beta(3)-adrenergic receptor (AR) agonists. Several analogs demonstrated potent agonist activity at the beta(3)-AR, fun
Autor:
Karen M. Ward, Mary Butler, Denise Gautreau, Subas M. Sakya, Joseph DiBrino, Jeff S. Lizano, Colin R. Rose, David A. Griffith, Shawn C Black, John R. Hadcock, Darrin Dutcher, Rebecca E. O’Connor, Dawn Kelly-Sullivan, Philip A. Iredale, Dennis O. Scott, Demetria B. DeBartolo, Philip A. Carpino, Michael Fichtner, Robert L. Dow, Michelle A. Sands, Robert F. Day
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(3)
A series of conformationally constrained bicyclic derivatives derived from SR141716 was prepared and evaluated as hCB(1)-R antagonists and inverse agonists. Optimization of the structure-activity relationships around the 2,6-dihydro-pyrazolo[4,3-d]py