Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Erol K. Bayburt"'
Autor:
Philip R. Kym, Arthur Gomtsyan, Gregory A. Gfesser, Bin Li, Regina M. Reilly, Bruce Clapham, Jerome F. Daanen, Rodger F. Henry, Torben R. Neelands, Pamela S. Puttfarcken, Susan M. Huang, Robert G. Schmidt, Robert J. Altenbach, S.K. Joshi, Huaqing Liu, Marlon D. Cowart, David N. Whittern, Phil B. Cox, Jill-Desiree Brederson, Michael J. Dart, Anurupa Shrestha, Donna Gauvin, Michael E. Kort, Erol K. Bayburt, Ping Song, Steve McGaraughty, Connie R. Faltynek, Heath A. McDonald, Patricia N. Banfor, Diana Schmidt, Eric A. Voight, Mohamad Shebley, Jason A. Segreti
Publikováno v:
Journal of Medicinal Chemistry. 59:4926-4947
Transient receptor potential vanilloid 3 (TRPV3) is a Ca(2+)- and Na(+)-permeable channel with a unique expression pattern. TRPV3 is found in both neuronal and non-neuronal tissues, including dorsal root ganglia, spinal cord, and keratinocytes. Recen
Autor:
Jerome F. Daanen, Joseph P. Mikusa, Chih Hung Lee, Chengmin Zhong, Jason A. Segreti, Patrick W. Mantyh, Torben R. Neelands, Patricia N. Banfor, Michael F. Jarvis, Arthur Gomtsyan, Prasant Chandran, Molly A. Sevcik, Philip R. Kym, Donna M. Gauvin, Regina M. Reilly, Kennan C. Marsh, Michael E. Kort, Connie R. Faltynek, James P. Sullivan, Erol K. Bayburt, Carol S. Surowy, Joseph R. Ghilardi, Prisca Honore, Gricelda Hernandez, Ryan M. Fryer, Shailen K. Joshi
Publikováno v:
Pain. 142:27-35
Transient receptor potential vanilloid type 1 (TRPV1) is a ligand-gated ion channel that functions as an integrator of multiple pain stimuli including heat, acid, capsaicin and a variety of putative endogenous lipid ligands. TRPV1 antagonists have be
Autor:
Carol S. Surowy, Katharine L. Chu, Prisca Honore, Rachid El Kouhen, Connie R. Faltynek, Bruce R. Bianchi, Ping Han, James P. Sullivan, Steve McGaraughty, Wende Niforatos, Arthur Gomtsyan, Erol K. Bayburt, Chih-Hung Lee, Torben R. Neelands, Heath A. McDonald, Melissa H. Vos, Michael F. Jarvis
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 326:879-888
The transient receptor potential vanilloid (TRPV) 1 receptor, a nonselective cation channel expressed on peripheral sensory neurons and in the central nervous system, plays a key role in pain. TRPV1 receptor antagonism is a promising approach for pai
Autor:
Prisca Honore, Connie R. Faltynek, James P. Sullivan, Jill M. Wetter, Arthur Gomtsyan, Michael F. Jarvis, Carol S. Surowy, Steven M. Hannick, Robert G. Schmidt, Erol K. Bayburt, Chih-Hung Lee, Kennan C. Marsh, Heath A. McDonald
Publikováno v:
Journal of Medicinal Chemistry. 51:392-395
Vanilloid receptor TRPV1 is a cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective antagonists is under investigation by several pharmaceutical compani
Autor:
Connie R. Faltynek, Joe Mikusa, Richard J. Perner, Jill M. Wetter, Stanley Didomenico, Tammie K. Jinkerson, Kennan C. Marsh, Chih-Hung Lee, John R. Koenig, Heath A. McDonald, Sean C. Turner, Arthur Gomtsyan, Erol K. Bayburt, Carol S. Surowy, Irene Drizin, Ryan G. Keddy, Prisca Honore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3894-3899
SAR studies for N-aryl-N′-benzyl urea class of TRPV1 antagonists have been extended to cover α-benzyl alkylation. Alkylated compounds showed weaker in vitro potencies in blocking capsaicin activation of TRPV1 receptor, but possessed improved pharm
Autor:
Kurill Lukin, Jill M. Wetter, Michael F. Jarvis, Guo Zhu Zheng, Joe Mikusa, Richard J. Perner, Erol K. Bayburt, Ryan G. Keddy, Robert G. Schmidt, Tammie K. Jinkerson, Connie R. Faltynek, Prisca Honore, John R. Koenig, Chih-Hung Lee, Arthur Gomtsyan, Stanley Didomenico, Irene Drizin, Heath A. McDonald, Sean C. Turner, Kennan C. Marsh, Karen St. George, Brian S. Brown
Publikováno v:
Journal of Medicinal Chemistry. 50:3651-3660
The synthesis and structure-activity relationship of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 (TRPV1) antagonists are described. A variety of cyclic amine substituents are well tolerated at the 4-position of the benzy
Autor:
Torben R. Neelands, C. Zhong, Erol K. Bayburt, B. Brown, Prisca Honore, Joseph P. Mikusa, W. Niforatos, Donna M. Gauvin, Gricelda Hernandez, H. McDonald, Michael W. Decker, Robert B. Moreland, Arthur Gomtsyan, Kennan C. Marsh, B. Bianchi, Prasant Chandran, Connie R. Faltynek, James P. Sullivan, C.-H. Lee, M. Cui
Publikováno v:
The Journal of Neuroscience. 26:9385-9393
Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. In addition to expression in primary affe
Autor:
Erol K. Bayburt, Prisca Honore, Tammie K. Jinkerson, Chih-Hung Lee, Heath A. McDonald, Sean C. Turner, Brian S. Brown, Irene Drizin, Kennan C. Marsh, James S. Polakowski, Jason A. Segreti, Michael F. Jarvis, John R. Koenig, Stanley Didomenico, Richard J. Perner, Jill M. Wetter, Guo Zhu Zheng, Carol T. Wismer, Ryan G. Keddy, Robert G. Schmidt, Connie R. Faltynek, Arthur Gomtsyan
Publikováno v:
Bioorganic & Medicinal Chemistry. 14:4740-4749
Novel 5,6-fused heteroaromatic ureas were synthesized and evaluated for their activity as TRPV1 antagonists. It was found that 4-aminoindoles and indazoles are the preferential cores for the attachment of ureas. Bulky electron-withdrawing groups in t
Autor:
Meiqun Jiang, Stanley Didomenico, Ronald D. Snyder, Karen M. Alexander, Shripad S. Bhagwat, Guo Zhu Zheng, Carol T. Wismer, Haixia Yu, Andrew O. Stewart, Marilyn S. Diehl, Gregory A. Gfesser, Kennan C. Marsh, Erol K. Bayburt, Robin R. Frey, Mark A. Matulenko, Marlon D. Cowart, Jeffery A. McKie, Arthur Gomtsyan, Kathy L. Kohlhaas, Michael F. Jarvis, Elizabeth A. Kowaluk, Joseph P. Mikusa, Steve McGaraughty, Chih-Hung Lee
Publikováno v:
Bioorganic & Medicinal Chemistry. 13:3705-3720
4-Amino-5,7-disubstituted pyridopyrimidines are potent, non-nucleoside inhibitors of adenosine kinase (AK). We recently identified a potent, orally efficacious analog, 4 containing a 7-pyridylmorpholine substituted ring system as the key structural e
Autor:
Kathy L. Kohlhaas, Richard J. Perner, Chih-Hung Lee, Erol K. Bayburt, Karen M. Alexander, Michael F. Jarvis, Elizabeth L. Kowaluk, Shripad S. Bhagwat, Gu Yu-Gui, Meiqun Jiang, Stanley Didomenico
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:2803-2807
The synthesis and structure-activity relationship of a series of 6,7-disubstituted 4-aminopyrido[2,3-d]pyrimidines as novel non-nucleoside adenosine kinase inhibitors is described. A variety of substituents, primarily aryl, at the C6 and C7 positions