Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Irene Drizin"'
Autor:
Brett Antonio, Robert J. Gregg, Gricelda H. Simler, Matthew S Johnson, Yi Liu, Dong Liu, Marc J. C. Scanio, Prisca Honore, Alison Knox, James B. Thomas, Shailen K. Joshi, Mark L. Chapman, Brian E. Marron, Irene Drizin, Douglas S. Krafte, Connie R. Faltynek, Robert N. Atkinson, Xu-Feng Zhang, Michael J. Krambis, Kort Michael E, Michael F. Jarvis, Stephen Werness, Kennan C. Marsh, Lei Shi, Char-Chang Shieh
Publikováno v:
Bioorganic & Medicinal Chemistry. 18:7816-7825
Na(v)1.8 (also known as PN3) is a tetrodotoxin-resistant (TTx-r) voltage-gated sodium channel (VGSC) that is highly expressed on small diameter sensory neurons. It has been implicated in the pathophysiology of inflammatory and neuropathic pain, and w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0ebd1fee852efa5ef6ea85bd394f0b15
https://doi.org/10.1016/j.bmc.2010.09.057
https://doi.org/10.1016/j.bmc.2010.09.057
Autor:
Rosemarie Roeloffs, Stephen Werness, Brian E. Marron, Chengmin Zhong, Brett Antonio, Ahmed H. Hakeem, Irene Drizin, Char-Chang Shieh, Mark L. Chapman, Joseph P. Mikusa, Marc J. C. Scanio, James B. Thomas, Shailen K. Joshi, Dong Liu, Mark A. Matulenko, Douglas S. Krafte, Robert N. Atkinson, Lei Shi, Kennan C. Marsh, Gricelda H. Simler, Matthew S Johnson, Michael J. Krambis, Kort Michael E, Michael F. Jarvis, Xu-Feng Zhang, Robert J. Gregg, Connie R. Faltynek, Matthew A. Secrest, Prisca Honore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6812-6815
A series of aryl-substituted nicotinamide derivatives with selective inhibitory activity against the Na(v)1.8 sodium channel is reported. Replacement of the furan nucleus and homologation of the anilide linker in subtype-selective blocker A-803467 (1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2a0d6b9da5e44daf33aabb753a354c07
https://doi.org/10.1016/j.bmcl.2010.08.121
https://doi.org/10.1016/j.bmcl.2010.08.121
Autor:
Matthew S Johnson, Dong Liu, Robert J. Gregg, Irene Drizin, Michael F. Gross, Gricelda Hernandez, Kennan C. Marsh, James B. Thomas, Mark L. Chapman, Chang Z. Zhu, Brian E. Marron, Connie R. Faltynek, Shailen K. Joshi, Prisca Honore, Stephen Werness, Michael E. Kort, Douglas S. Krafte, Robert N. Atkinson, Rosemarie Roeloffs, William A. Carroll, Marc J. C. Scanio, Xu-Feng Zhang, Donna M. Gauvin, Michael J. Krambis, Michael F. Jarvis, Char-Chang Shieh, Lei Shi, Joseph P. Mikusa
Publikováno v:
Bioorganic & Medicinal Chemistry. 16:6379-6386
The synthesis and pharmacological characterization of a novel furan-based class of voltage-gated sodium channel blockers is reported. Compounds were evaluated for their ability to block the tetrodotoxin-resistant sodium channel Na(v)1.8 (PN3) as well
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4bdfd333e1e1c8103d37b0c3b7e0a15f
https://doi.org/10.1016/j.bmc.2008.05.003
https://doi.org/10.1016/j.bmc.2008.05.003
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b94d6173302f6adb4d15301008d5dc2f
https://doi.org/10.1016/j.bmcl.2007.04.105
https://doi.org/10.1016/j.bmcl.2007.04.105
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9c0ad2a8944bd1b86fe961f36808a25e
https://doi.org/10.1021/jm070276i
https://doi.org/10.1021/jm070276i
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c45dbc1d75427630fd0170c805218c2c
https://doi.org/10.1016/j.bmc.2006.03.027
https://doi.org/10.1016/j.bmc.2006.03.027
Publikováno v:
Synthetic Communications. 34:557-565
5‐Amino‐2H‐pyran‐3(6H)‐one, 1, is a novel intermediate that is useful in the synthesis of pyran containing dihydropyridines. The synthesis and use of 1 will be discussed.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::754de90257b87b93cd364d84fe47140f
https://doi.org/10.1081/scc-120027702
https://doi.org/10.1081/scc-120027702
Autor:
Irene Drizin, Jorge D. Brioni, Michael E. Kort, Hao Bai, Michael C. Fitzgerald, Robert J. Gregg, Linda L. King, Robert J. Altenbach, William A. Carroll, Lin Yi, Michael J. Coghlan, Rodger F. Henry, Rui Tang, Anthony V. Daza, Henry Zhang, Murali Gopalakrishnan, Michael E. Brune, Steven A. Buckner, Kristi L. Whiteaker, Thomas A. Fey, Sean C. Turner, Christopher Cassidy, Mark W. Holladay, Yiyuan Chen, Philip R. Kym, Ivan Milicic, James P. Sullivan
Publikováno v:
Journal of Medicinal Chemistry. 47:3163-3179
Structure−activity relationships were investigated on a novel series of sulfonyldihydropyridine-containing KATP openers. Ring sizes, absolute stereochemistry, and aromatic substitution were evaluated for KATP activity in guinea pig bladder cells us
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::48701963d5335233e58180eb726e63f5
https://doi.org/10.1021/jm030356w
https://doi.org/10.1021/jm030356w
Autor:
Kristi L. Whiteaker, Steven A. Buckner, James P. Sullivan, Sujatha M. Gopalakrishnan, Zhang Henry Q, Mark W. Holladay, Murali Gopalakrishnan, William A. Carroll, Lin Yi, Irene Drizin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1481-1484
A novel series of tricyclic dihydropyrimidines was synthesized and evaluated for activity as K(ATP) channel openers. The functional activity of several compounds, for example 6A (EC(50)=30nM) and its enantiomers exceeded cromakalim.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e8712ef75a8bebbfb8d1ced23a0d10e3
https://doi.org/10.1016/s0960-894x(02)00207-x
https://doi.org/10.1016/s0960-894x(02)00207-x
Autor:
Irene Drizin, et al. et al.
Publikováno v:
ChemInform. 33
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c7f36fd614fe81480281b3376485154d
https://doi.org/10.1002/chin.200238238
https://doi.org/10.1002/chin.200238238