Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Carolyn Diane Dzierba"'
Autor:
Jodi K. Muckelbauer, Ramkumar Rajamani, Jeffrey M. Brown, C M Vijaya Kumar, Kumaran Dandapani, Jonathan Lippy, Saravanan Elavazhagan, Vijay T. Ahuja, John E. Macor, Carolyn Diane Dzierba, Brian D. Hamman, Walter Kostich, Michael Gulianello, Manoj Dokania, Susan E. Kiefer, Susheel J. Nara, Joanne J. Bronson, Amy Easton, Richard A. Hartz, Linda J. Bristow, Martin A. Lewis, Jason Allen, Sreenivasulu N Pattipati, Neha Surti, Lisa Hunihan, Daniel M. Camac
Publikováno v:
Journal of medicinal chemistry. 64(15)
Effective treatment of chronic pain, in particular neuropathic pain, without the side effects that often accompany currently available treatment options is an area of significant unmet medical need. A phenotypic screen of mouse gene knockouts led to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a874893d7c1ec730ba639d989c3f7ccd
https://pubmed.ncbi.nlm.nih.gov/34270254
https://pubmed.ncbi.nlm.nih.gov/34270254
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:
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:
James E. Grace, Brian Zambrowicz, Pradeep Vattikundala, Kenneth G. Carson, Jonathan Lippy, Clotilde Bourin, Alan Main, Alan Wilson, Sreenivasulu Naidu, Sandhya Mandlekar, Carolyn Diane Dzierba, Saravanan Elavazhagan, Walter Kostich, Gauri Shankar, Jeffrey M. Brown, Charles M. Conway, Charles F. Albright, Justin Vijay Louis, Yu-Wen Li, Vivek Sharma, Yanling Huang, Laszlo Kiss, Amr Nouraldeen, Susheel J. Nara, Martin A. Lewis, Ryan Westphal, Vinay K. Holenarsipur, Anand Balakrishnan, Amy Easton, Robert Zaczek, Jonathan C. Swaffield, Ted Molski, Rick L. Pieschl, Kevin Baker, Katerina Savelieva, Yingzhi Bi, Kenneth S. Santone, Linda J. Bristow, John E. Macor, Jianlin Feng, Guilan Ye, Joanne J. Bronson, Manish Lal Das, Reeba K. Vikramadithyan, Kevin O’Malley, Jason W. Allen, Brian D. Hamman, Michael Gulianello, Yifeng Lu, Thomas H. Lanthorn, Kimberley A. Lentz, Anoop Kumar, Manoj Dokania, Kumaran Dandapani, Rex Denton
Publikováno v:
The Journal of Pharmacology and Experimental Therapeutics
To identify novel targets for neuropathic pain, 3097 mouse knockout lines were tested in acute and persistent pain behavior assays. One of the lines from this screen, which contained a null allele of the adapter protein-2 associated kinase 1 (AAK1) g
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::04b1480bd30607a9fe64d0e01fbd6b27
http://europepmc.org/articles/PMC4998676
http://europepmc.org/articles/PMC4998676
Autor:
Zhi Liang, Alan Wilson, Li Dong, Neil T. Burford, David S. Kimball, Kenneth G. Carson, Yingzhi Bi, Yulian Zhang, Bireshwar Dasgupta, Carolyn Diane Dzierba, Richard A. Hartz, James E. Grace, G. Greg Zipp, Soojin Kwon, Martin A. Lewis, Joanne J. Bronson, Cynthia Anne Fink, Amr Nouraldeen, Saadat Aleem, Giovanni Cianchetta, Jiancheng Wang, Ying Liu, Vijay T. Ahuja, Robert L. Bertekap, Jianxin Han, Michael Alan Green, Angela Cacace, Godwin Kumi, Yudith Garcia, Ying Qiao, Meredith Ferrante, John E. Macor, Ryan Westphal
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:1448-1452
Small molecule modulators of GPR88 activity (agonists, antagonists, or modulators) are of interest as potential agents for the treatment of a variety of psychiatric disorders including schizophrenia. A series of phenylglycinol and phenylamine analogs
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16bf15e7cd2cc6067dbe9746466df095
https://doi.org/10.1016/j.bmcl.2015.01.036
https://doi.org/10.1016/j.bmcl.2015.01.036
Autor:
Debra J. Post-Munson, Clotilde Bourin, Carolyn Diane Dzierba, Ling Chen, Michele Matchett, John D. Graef, Ronald J. Knox, Kimberly Newberry, Guanglin Luo, James B Herrington, Amy Newton, Matthew G. Soars, Arun K. Senapati, Kathy Mosure, Nicholas A. Meanwell, Digavalli V. Sivarao, Shuya Wang, Rick L. Pieschl, Linda J. Bristow, Eric Shields, Lorin A. Thompson, Amy Easton
Publikováno v:
Journal of Medicinal Chemistry. 62:2213-2213
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::43b1cafdbe761a2ee2b84d1a8c68e354
https://doi.org/10.1021/acs.jmedchem.9b00202
https://doi.org/10.1021/acs.jmedchem.9b00202