Zobrazeno 1 - 10
of 37
pro vyhledávání: '"Rick L, Pieschl"'
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:
Kurex Sidik, Matthew Fronheiser, Yu-Wen Li, Adrienne Pena, Feng Luo, Linda J. Bristow, Patrick L Chow, Haiying Tang, Rick L. Pieschl, Daniel W. Kukral, Gabriel Tobon, Harold Malone, Wendy Hayes
Publikováno v:
Journal of Psychopharmacology. 32:146-155
Major depressive disorder is a leading cause of disability globally. Improvements in the efficacy of antidepressant therapy are needed as a high proportion (>40%) of individuals with major depressive disorder fail to respond adequately to current tre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e832e7809474697376ad4f68971c22ee
https://doi.org/10.1177/0269881117746901
https://doi.org/10.1177/0269881117746901
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:
Mahesh Paschapur, Jeffrey M. Brown, Tanmaya Bastia, Lawrence R. Marcin, Jayakumar Sankara Warrier, Srinivasan Thangathirupathy, Joanne J. Bronson, Raja Reddy Kallem, Huiping Zhang, Jyoti Gulia, Alda Fernandes, Digavalli V. Sivarao, Deborah Keavy, Amy Newton, Jianqing Li, Pattipati S. Naidu, Kuchibhotla Vijaya Kumar, James Kempson, Michael R. Weed, Rick L. Pieschl, Mark Bookbinder, Charlie F. Albright, Kimberly Newberry, Yu-Wen Li, Dalton King, Manjunath Ramarao, Jean Simmermacher, Linda J. Bristow, Meenakshee Sinha, Eric Shields, Lorin A. Thompson, John E. Macor, Charulatha Sanmathi, Imadul Islam, B.N. Srikumar, Richard E. Olson, John D. Graef, Arvind Mathur, Narasimharaju Kalidindi, Joseph Polino, Michael Sinz, Thaddeus F. Molski, Jayant Aher, Reeba K. Vikramadithyan
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 363:377-393
(R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one (BMS-986169) and the phosphate prodrug 4-((3S,4S)-3-fluoro-1-((R)-1-(4-methylbenzyl)-2-oxopyrrolidin-3-yl)piperidin-4-yl)phenyl dihydrogen phosphate (BMS-98
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1fc12be7607ec5d5401f625fdca24cd2
https://doi.org/10.1124/jpet.117.242784
https://doi.org/10.1124/jpet.117.242784
Autor:
David R. Langley, Rick L. Pieschl, John Watson, Simon Low, Linda J. Bristow, Debra J. Post-Munson, Michael K. Ahlijanian, Ramkumar Rajamani, Sophie Wu, James Herrington, Mian Gao, Lisa Megson, Iyoncy Rodrigo, David L. Wensel
Publikováno v:
Molecular Pharmacology. 92:310-317
The NaV1.7 voltage-gated sodium channel is implicated in human pain perception by genetics. Rare gain of function mutations in NaV1.7 lead to spontaneous pain in humans whereas loss of function mutations results in congenital insensitivity to pain. H
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::07940ab23c226013ba900bf2c7333fa2
https://doi.org/10.1124/mol.117.108712
https://doi.org/10.1124/mol.117.108712
Autor:
Justin Vijay Louis, Kumaran Dandapani, Susheel J. Nara, Yang Hong, Yung Tian, Sarat Kumar Sarvasiddhi, Yifeng Lu, Carolyn Diane Dzierba, Walter Kostich, Yu-Wen Li, Rick L. Pieschl, Sreenivasulu Naidu, Charlie F. Albright, Joanne J. Bronson, John E. Macor, Reeba K. Vikramadithyan
Publikováno v:
Neuropharmacology. 118:167-174
Adaptor-associated kinase 1 (AAK1), a member of the Ark1/Prk1 family of serine/threonine kinases, plays a role in modulating clatherin coated endocytosis of specific surface receptors. We have demonstrated that AAK1 inhibitors are efficacious in rode
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f168813c715e6b8c8865371b20f68a5c
https://doi.org/10.1016/j.neuropharm.2017.03.015
https://doi.org/10.1016/j.neuropharm.2017.03.015
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