Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Christopher, Walpole"'
Autor:
Wei Zhongyong, Johan Broddefalk, Madeleine Antonsson, Kosrat Amin, Jörgen Jensen, Johan Ulander, Maxime Tremblay, Stephane St-Onge, Karolina Nilsson, Shujuan Jin, Anders Lehmann, Alleyn T. Plowright, Christopher Walpole, Tomaszewski Miroslaw, Hua Yang
Publikováno v:
Journal of Medicinal Chemistry. 56:220-240
Agonists of the cannabinoid receptor 1 (CB1) have been suggested as possible treatments for a range of medical disorders including gastroesophageal reflux disease (GERD). While centrally acting cannabinoid agonists are known to produce psychotropic e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d7e05819466ec51f70ae07e9321387a5
https://doi.org/10.1021/jm301511h
https://doi.org/10.1021/jm301511h
Autor:
Mickaël Maudet, Jennifer M. A. Laird, Ronald Zemribo, Paul Jones, Michael Dabrowski, Andis Slaitas, Yevgeni Besidski, Gitte Terp, Karin Kolmodin, Andrea Penwell, Andrew Griffin, Didier Rotticci, Anna K. Sundgren-Andersson, Christopher Walpole, Dean Johnson, Alexander Munro, Yin Hu, Therese Lundström, Maryse Labarre, Inger Kers, Huascar Villanueva, Johan Bylund, Martin Nylöf, Mats Svensson, Denis Labrecque, Magali Harter, Sandrine Leclerc, William Brown, Sophie Dautrey, Shawn Johnstone, John Martino, Lucy Horoszok
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:6205-6211
Benzothiazole amides were identified as TRPV1 antagonists from high throughput screening using recombinant human TRPV1 receptor and structure-activity relationships were explored to pinpoint key pharmacophore interactions. By increasing aqueous solub
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5999ae8c775dbcf4f87b0f920411e95
https://doi.org/10.1016/j.bmcl.2012.08.018
https://doi.org/10.1016/j.bmcl.2012.08.018
Autor:
Xuehong Luo, Xiao Hong Yu, Pourashraf Mehrnaz, Sanjay Srivastava, Dominic Salois, Cheng Yun-Xing, Kemal Payza, Christopher Walpole, Etienne Lessard, Stephane St-Onge, Tomaszewski Miroslaw
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1619-1624
An oral, peripherally restricted CB1/CB2 agonist could provide an interesting approach to treat chronic pain by harnessing the analgesic properties of cannabinoids but without the well-known central side effects. γ-Carbolines are a novel class of po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a70c2a778db169330114c41d0ed05f33
https://doi.org/10.1016/j.bmcl.2011.12.124
https://doi.org/10.1016/j.bmcl.2011.12.124
Autor:
Martin Coupal, Paul Jones, Lejla Hodzic, Wenhau Xiao, Edward Roberts, Andrew Griffin, Daniel Delorme, Dominic Salois, Maryse Labarre, Stephane St-Onge, Christopher Walpole, Jamie Boulet, Lars Gawell, Rico Lavoie, Joanne Butterworth, William Brown
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5994-5998
We have investigated a series of phenolic diaryl amino piperidine delta opioid receptor agonists, establishing the importance of the phenol functional group and substitution on the piperdine nitrogen for delta agonist activity and selectivity versus
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::309cc40e144f4ea22f0ebf8874c89c2d
https://doi.org/10.1016/j.bmcl.2009.09.072
https://doi.org/10.1016/j.bmcl.2009.09.072
Autor:
William Brown, Tomaszewski Miroslaw, Etienne Lessard, Christopher Walpole, Wei Zhongyong, Hua Yang, Beha Sara, Sanjay Srivastava, Maxime Tremblay, Shi Yi Yue, Shawn Johnstone, Stephane St-Onge, Thierry Groblewski, Anne-Julie Archambault, Ziping Liu, Page Daniel
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(12)
Cannabinoid CB1 receptor agonists exhibit potent analgesic effects in rodents and humans, but their clinical utility as analgesic drugs is often limited by centrally mediated side effects. We report herein the preparation of N-methyl-3-(tetrahydro-2H
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8398b5e47f84620dc49296ccdf8d606e
https://pubmed.ncbi.nlm.nih.gov/22607668
https://pubmed.ncbi.nlm.nih.gov/22607668
Autor:
Eric Grazzini, Carmen Leung, Michel Paré, Louis-David Cantin, Vijayaratnam Santhakumar, Giovanni Martino, Kemal Payza, Jean Labrecque, Tomaszewski Miroslaw, Christophe Buon, Yun-Jin Hu, Nirvana Popovic, Malken Bayrakdarian, Xuehong Luo, Xiao Hong Yu, Christopher Walpole, Denis Projean
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(7)
Purinergic receptor P2X3 has been linked to analgesia in a number of pre-clinical models of pain, and is expressed in the human pain perception pathway. Only few P2X3-selective antagonists have been reported to date. This Letter describes the SAR and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ac580afe3a8c93e8366c071f95163f37
https://pubmed.ncbi.nlm.nih.gov/22370269
https://pubmed.ncbi.nlm.nih.gov/22370269
Autor:
Marie Roumi, Dominic Salois, Christopher Walpole, Lynda Adam, William Brown, Mylene Gosselin, Pierre-Emmanuel Morin, Andrew Griffin, Martin Coupal
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(21)
We have investigated phenol replacements in a series of diaryl amino piperidine delta opioid agonists. From this study we have demonstrated that the hydroxy functional group can be replaced with a primary amide group, giving enhanced activity at the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4509e8ae81550e436ca52392014d70e4
https://pubmed.ncbi.nlm.nih.gov/19800790
https://pubmed.ncbi.nlm.nih.gov/19800790
Autor:
Lejla Hodzic, Martin Coupal, Chris Dockendorff, Lautens Mark, Christopher Walpole, Nathan Spear, Shujuan Jin, Madeline Olsen, Kemal Payza, Tomaszewski Miroslaw
Publikováno v:
ChemInform. 40
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::cdb59135be6e25ab750125e933f51b97
https://doi.org/10.1002/chin.200929090
https://doi.org/10.1002/chin.200929090
Autor:
Lejla Hodzic, Chris Dockendorff, Tomaszewski Miroslaw, Shujuan Jin, Christopher Walpole, Mark Lautens, Nathan Spear, Martin Coupal, Kemal Payza, Madeline Olsen
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(4)
A series of 1-aminotetralin scaffolds was synthesized via metal-catalyzed ring-opening reactions of heterobicyclic alkenes. Small libraries of amides and amines were made using the amino group of each scaffold as a handle. Screening of these librarie
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::25fd755b051ca8bffc9bfc1ffc5681aa
https://pubmed.ncbi.nlm.nih.gov/19168350
https://pubmed.ncbi.nlm.nih.gov/19168350
Autor:
Daniel, Pagé, Elise, Balaux, Luc, Boisvert, Ziping, Liu, Claire, Milburn, Maxime, Tremblay, Zhongyong, Wei, Simon, Woo, Xuehong, Luo, Yun-Xing, Cheng, Hua, Yang, Sanjay, Srivastava, Fei, Zhou, William, Brown, Miroslaw, Tomaszewski, Christopher, Walpole, Leila, Hodzic, Stéphane, St-Onge, Claude, Godbout, Dominic, Salois, Kemal, Payza, Keymal, Payza
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(13)
The preparation and evaluation of a novel class of CB2 agonists based on a benzimidazole moiety are reported. They showed binding affinities up to 1 nM towards the CB2 receptor with partial to full agonist potencies. They also demonstrated good to ex
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b38faeba6c5ce18da2d54a009c6fb34
https://pubmed.ncbi.nlm.nih.gov/18522867
https://pubmed.ncbi.nlm.nih.gov/18522867