Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Michele Matchett"'
Autor:
Carolyn Diane Dzierba, Linda J. Bristow, Ramkumar Rajamani, Jie Chen, Rick L. Pieschl, Sing-Yuen Sit, Brian Lee Venables, Michele Matchett, Ronald J. Knox, Lorin A. Thompson, Nicholas A. Meanwell, Yong-Jin Wu, Jason M. Guernon, James Herrington
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:659-663
Screening of 100 acylsulfonamides from the Bristol-Myers Squibb compound collection identified the C3-cyclohexyl indole 6 as a potent Nav1.7 inhibitor. Replacement of the C2 furanyl ring of 6 with a heteroaryl moiety or truncation of this group led t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2f347d20e2f2ebee9e7e423555c27787
https://doi.org/10.1016/j.bmcl.2018.12.013
https://doi.org/10.1016/j.bmcl.2018.12.013
Autor:
Carolyn Diane Dzierba, Debra J. Post-Munson, Ronald J. Knox, Lorin A. Thompson, Shuya Wang, Matthew G. Soars, Michele Matchett, Linda J. Bristow, James Herrington, Clotilde Bourin, Amy Newton, Rick L. Pieschl, Eric Shields, Amy Easton, Kathy Mosure, Guanglin Luo, Kimberly Newberry, Ling Chen, John D. Graef, Arun K. Senapati, Nicholas A. Meanwell, Digavalli V. Sivarao
Publikováno v:
Journal of Medicinal Chemistry. 62:831-856
3-Aryl-indole and 3-aryl-indazole derivatives were identified as potent and selective Nav1.7 inhibitors. Compound 29 was shown to be efficacious in the mouse formalin assay and also reduced complete Freund’s adjuvant (CFA)-induced thermal hyperalge
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8738aee38a77abf37b839d8d841c0ca8
https://doi.org/10.1021/acs.jmedchem.8b01550
https://doi.org/10.1021/acs.jmedchem.8b01550
Autor:
Nicholas A. Meanwell, Kevin J. Robbins, Carolyn Diane Dzierba, Rick L. Pieschl, Ramkumar Rajamani, James Herrington, Lorin A. Thompson, Andrea McClure, Yong-Jin Wu, Michele Matchett, Ronald J. Knox, Brian Lee Venables, Jason M. Guernon, Linda J. Bristow, Richard E. Olson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:958-962
Replacement of the piperidine ring in the lead benzenesulfonamide Nav1.7 inhibitor 1 with a weakly basic morpholine core resulted in a significant reduction in Nav1.7 inhibitory activity, but the activity was restored by shortening the linkage from m
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e7ad493840369e26cbfb8ea5aabd0b90
https://doi.org/10.1016/j.bmcl.2018.01.035
https://doi.org/10.1016/j.bmcl.2018.01.035
Autor:
Kathleen W. Mosure, Michele Matchett, Ronald J. Knox, Richard E. Olson, Joanne J. Bronson, Nicholas A. Meanwell, Matthew G. Soars, Linda J. Bristow, Ramkumar Rajamani, James Herrington, Amy Easton, Digavalli V. Sivarao, Dawn D. Parker, Rick L. Pieschl, Ping Chen, Guanglin Luo, Omar S. Barnaby, Lorin A. Thompson, Yong-Jin Wu, Andrea McClure, Jason M. Guernon, Amy Newton, Alicia Ng, Clotilde Bourin, Carolyn Diane Dzierba
Publikováno v:
Bioorganic & Medicinal Chemistry. 25:5490-5505
Since zwitterionic benzenesulfonamide Nav1.7 inhibitors suffer from poor membrane permeability, we sought to eliminate this characteristic by replacing the basic moiety with non-basic bicyclic acetals and monocyclic ethers. These efforts led to the d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::120b30199f8465162b72cfc311e05f8b
https://doi.org/10.1016/j.bmc.2017.08.012
https://doi.org/10.1016/j.bmc.2017.08.012
Autor:
Debra J. Post-Munson, Amy Easton, Carolyn Diane Dzierba, Amy Newton, Yong-Jin Wu, Ronald J. Knox, Kevin J. Robbins, Jason M. Guernon, Clotilde Bourin, Ramkumar Rajamani, Richard E. Olson, James Herrington, Michele Matchett, Kimberly Newberry, John D. Graef, Jianliang Shi, Lorin A. Thompson, Shuya Wang, Jonathan L. Ditta, Nicholas A. Meanwell, Rick L. Pieschl, Matthew G. Soars, Linda J. Bristow, Kathleen W. Mosure
Publikováno v:
Journal of Medicinal Chemistry. 60:2513-2525
By taking advantage of certain features in piperidine 4, we developed a novel series of cyclohexylamine- and piperidine-based benzenesulfonamides as potent and selective Nav1.7 inhibitors. However, compound 24, one of the early analogs, failed to red
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::70eeeaf9d44c1cee668426b1f9c6fa0f
https://doi.org/10.1021/acs.jmedchem.6b01918
https://doi.org/10.1021/acs.jmedchem.6b01918
Autor:
Guanglin, Luo, Ling, Chen, Amy, Easton, Amy, Newton, Clotilde, Bourin, Eric, Shields, Kathy, Mosure, Matthew G, Soars, Ronald J, Knox, Michele, Matchett, Rick L, Pieschl, Debra J, Post-Munson, Shuya, Wang, James, Herrington, John, Graef, Kimberly, Newberry, Digavalli V, Sivarao, Arun, Senapati, Linda J, Bristow, Nicholas A, Meanwell, Lorin A, Thompson, Carolyn, Dzierba
Publikováno v:
Journal of medicinal chemistry. 62(4)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::65eb13dd58efb30cbfdb34202aa50d9e
https://pubmed.ncbi.nlm.nih.gov/30576602
https://pubmed.ncbi.nlm.nih.gov/30576602
Autor:
Valerie J. Whiterock, John E. Macor, Joanne J. Bronson, Melissa Hill-Drzewi, Regina Miller, Lizbeth Gallagher, Thaddeus F. Molski, Amy Easton, Xiaoliang Zhuo, Matthew D. Hill, Andrew P. Degnan, Xiaojun Han, Jeffrey M. Brown, Robert L. Bertekap, Haiquan Fang, Michael Gulianello, Michele Matchett, Kenneth S. Santone, Anand Balakrishnan
Publikováno v:
ACS Medicinal Chemistry Letters. 7:1082-1086
The metabotropic glutamate receptor 5 (mGluR5) is an attractive target for the treatment of schizophrenia due to its role in regulating glutamatergic signaling in association with the N-methyl-d-aspartate receptor (NMDAR). We describe the synthesis o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d90ae309c4691d80df7686005bbf768d
https://doi.org/10.1021/acsmedchemlett.6b00292
https://doi.org/10.1021/acsmedchemlett.6b00292
Autor:
Yong-Jin, Wu, Brian, Venables, Jason, Guernon, Jie, Chen, Sing-Yuen, Sit, Ramkumar, Rajamani, Ronald J, Knox, Michele, Matchett, Rick L, Pieschl, James, Herrington, Linda J, Bristow, Nicholas A, Meanwell, Lorin A, Thompson, Carolyn, Dzierba
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(4)
Screening of 100 acylsulfonamides from the Bristol-Myers Squibb compound collection identified the C3-cyclohexyl indole 6 as a potent Na
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::7e87a6b212eb6b55622d6c13aaa81742
https://pubmed.ncbi.nlm.nih.gov/30638874
https://pubmed.ncbi.nlm.nih.gov/30638874
Autor:
Yong-Jin, Wu, Jason, Guernon, Andrea, McClure, Brian, Venables, Ramkumar, Rajamani, Kevin J, Robbins, Ronald J, Knox, Michele, Matchett, Rick L, Pieschl, James, Herrington, Linda J, Bristow, Nicholas A, Meanwell, Richard, Olson, Lorin A, Thompson, Carolyn, Dzierba
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(5)
Replacement of the piperidine ring in the lead benzenesulfonamide Na
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::a945bed500393208c3e51c3857982302
https://pubmed.ncbi.nlm.nih.gov/29439904
https://pubmed.ncbi.nlm.nih.gov/29439904
Autor:
Yong-Jin, Wu, Jason, Guernon, Andrea, McClure, Guanglin, Luo, Ramkumar, Rajamani, Alicia, Ng, Amy, Easton, Amy, Newton, Clotilde, Bourin, Dawn, Parker, Kathleen, Mosure, Omar, Barnaby, Matthew G, Soars, Ronald J, Knox, Michele, Matchett, Rick, Pieschl, James, Herrington, Ping, Chen, D V, Sivarao, Linda J, Bristow, Nicholas A, Meanwell, Joanne, Bronson, Richard, Olson, Lorin A, Thompson, Carolyn, Dzierba
Publikováno v:
Bioorganicmedicinal chemistry. 25(20)
Since zwitterionic benzenesulfonamide Na
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::e80fb5093b3d1e69533ad8ff92e48500
https://pubmed.ncbi.nlm.nih.gov/28818462
https://pubmed.ncbi.nlm.nih.gov/28818462