Zobrazeno 1 - 4
of 4
pro vyhledávání: '"Stephanie Brumfield"'
Autor:
Zheng Tan, Steve Sorota, Deen Tulshian, R. Jason Herr, William G. Earley, Charles R. Heap, Stephanie Brumfield, Terry Bridal, Jennifer Hanisak, Xiaoping Zhou, Julius Matasi, Ana Bercovici, Ginny D. Ho, Diane Rindgen, Brandy Courneya, Shu-Wei Yang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:4110-4113
A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized and displayed potent Nav1.7 inhibitory activity and moderate selectivity over Nav1.5. The syntheses, structure-activity relationships, and selected pharmacokinetic data of these anal
Autor:
Julius J. Matasi, Stephanie Brumfield, Deen Tulshian, Michael Czarnecki, William Greenlee, Charles G. Garlisi, Hongchen Qiu, Kristine Devito, Shu-Cheng Chen, Youngliang Sun, Rosalia Bertorelli, William Geiss, Van-Duc Le, Gregory S. Martin, Samuel A. Vellekoop, James Haber, Melissa L. Allard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3805-3808
Structure-activity relationship (SAR) efforts around our initial lead compound 1 led to the identification of potent P2X(7) receptor antagonists with improved pharmacokinetic profiles. These compounds were potent and selective at the P2X(7) receptor
Autor:
Peter Korakas, Duane A. Burnett, Rosalia Bertorelli, Gianluca Lozza, Stephanie Brumfield, T.K. Sasikumar, Cheng Li, Angelo Reggiani, Chad Bennett, Martin S. Domalski, Lisa S. Silverman, Wen-Lian Wu, Li Qiang, Julius Matasi, Chad E. Knutson, Deen Tulshian, Mariagrazia Grilli, William J. Greenlee
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(23)
High throughput screening identified the pyridothienopyrimidinone 1 as a ligand for the metabotropic glutamate receptor 1 (mGluR1=10 nM). Compound 1 has an excellent in vivo profile; however, it displays unfavorable pharmacokinetic issues and metabol
Autor:
Stephanie Brumfield, Julius J. Matasi, Deen Tulshian, Michael Czarniecki, William Greenlee, Charles Garlisi, Hongchen Qiu, Kristine Devito, Shu-Cheng Chen, Yongliang Sun, Rosalia Bertorelli, Justin Ansell, William Geiss, Van-Duc Le, Gregory S. Martin, Samuel A. Vellekoop, James Haber, Melissa L. Allard
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(24)
Novel P2X(7) antagonists were developed using a purine scaffold. These compounds were potent and selective at the P2X(7) receptor in human and rodent as well as efficacious in rodent pain models. Compound 15a was identified to have oral potency in se