Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Stephen J. Medhurst"'
Autor:
Andrew Charlton, Stephen J. Medhurst, Laura J. Chambers, Livermore David, Brian Peter Slingsby, Andy Billinton, Lee William Page, Anton D. Michel, Daryl S. Walter, Jon Graham Anthony Steadman, Shilina Roman, Sadhana Patel, Elena Fonfria, Robert Gleave, Stefan Senger, Katharine Laura Collis, Andrew P. Moses, Sue D. Collins, Muna H. Abdi, Paul John Beswick, Clarisse L. Lejeune, David Kenneth Dean, Alexander J. Stevens
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5080-5084
A computational lead-hopping exercise identified compound 4 as a structurally distinct P2X(7) receptor antagonist. Structure-activity relationships (SAR) of a series of pyroglutamic acid amide analogues of 4 were investigated and compound 31 was iden
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9a3ff37009bb76b9bfd50c27c623c06d
https://doi.org/10.1016/j.bmcl.2010.07.033
https://doi.org/10.1016/j.bmcl.2010.07.033
Autor:
Andy Billinton, Sue Roomans, Stefan Senger, Anton D. Michel, Stephen J. Medhurst, Robert Gleave, Daryl S. Walter, Elena Fonfria, Laura J. Chambers, Andrew P. Moses, Shilina Roman, David Kenneth Dean, Alexander J. Stevens, Paul John Beswick, Sadhana Patel
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4653-4656
Structure–activity relationships (SAR) of analogues of lead compound 1 were investigated and compound 16 was selected for further study in animal models of pain. Compound 16 was shown to be a potent antihyperalgesic agent in both the rat acute comp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c05399c19e1a56ae550e1d9ced9f9a3a
https://doi.org/10.1016/j.bmcl.2010.05.107
https://doi.org/10.1016/j.bmcl.2010.05.107
Autor:
David Matthew Wilson, Alison M. Ray, Andrew D. Medhurst, Robert P. Davis, Ciaran M. Regan, Andrew G. Foley, Teresa Heslop, Sandrine Ociepka, Michael A. Briggs, Trevor White, Barry Crook, Barry Sidney Orlek, Stephen J. Medhurst, Andrew R. Calver, Brenda K. Trail, Iain P. Chessell, Becky Sargent, Tania O. Stean, Joanne Schogger, Neil Upton, Warren D. Hirst, Gordon Bruton, John B. Davis
Publikováno v:
Biochemical Pharmacology. 73:1182-1194
GSK207040 (5-[(3-cyclobutyl-2,3,4,5-tetrahydro-1 H -3-benzazepin-7-yl)oxy]- N -methyl-2-pyrazinecarboxamide) and GSK334429 (1-(1-methylethyl)-4-({1-[6-(trifluoromethyl)-3-pyridinyl]-4-piperidinyl}carbonyl)hexahydro-1 H -1,4-diazepine) are novel and s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9f6a376319db83a13187d88a7430b550
https://doi.org/10.1016/j.bcp.2007.01.007
https://doi.org/10.1016/j.bcp.2007.01.007
Autor:
Stephen J. Medhurst, Sadhana Patel, Peter McIntyre, Mohanjit Panesar, Katharine Walker, Alyson Fox, Laszlo Urban
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 304:56-62
Vanilloid receptor type 1 (VR1) (TRPV1) is a ligand-gated ion channel expressed on sensory nerves that responds to noxious heat, protons, and chemical stimuli such as capsaicin. Herein, we have examined the activity of the VR1 antagonist capsazepine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::85c3ead2f110926964f07a1e17f30733
https://doi.org/10.1124/jpet.102.042010
https://doi.org/10.1124/jpet.102.042010
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 42(7)
The simultaneous effects of the cytochrome P450 inhibitor 1-aminobenzotriazole (ABT) on inhibition of in vivo metabolism and gastric emptying were evaluated with the test compound 7-(3,5-dimethyl-1H-1,2,4-triazol-1-yl)-3-(4-methoxy-2-methylphenyl)-2,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62d78f3315eee4ec5f2915b580beee58
https://pubmed.ncbi.nlm.nih.gov/24727486
https://pubmed.ncbi.nlm.nih.gov/24727486
Autor:
Jon Graham Anthony Steadman, Daryl S. Walter, Beverley Smith, Lee Abberley, David Kenneth Dean, Elena Fonfria, Tiziana Scoccitti, Anton D. Michel, Sadhana Patel, Shilina Roman, Robert Gleave, Katharine Laura Collis, Stephen J. Medhurst, Andrew P. Moses, Aude Bebius, Paul John Beswick, Andy Billinton
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(22)
A backup molecule to compound 2 was sought by targeting the most likely metabolically vulnerable site in this molecule. Compound 18 was subsequently identified as a potent P2X(7) antagonist with very low in vivo clearance and high oral bioavailabilit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5cdb4b6ee4ecb8615e490657bc2ef801
https://pubmed.ncbi.nlm.nih.gov/20934331
https://pubmed.ncbi.nlm.nih.gov/20934331
Autor:
Iain Chessell, Jane P. Hughes, Sadhana Patel, Andy Billinton, Stephen J. Medhurst, Christopher N. Johnson, Z. Ali, Nick M. Clayton
Publikováno v:
European Journal of Pain. 13
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a7305daff0d068e7017bc858d79f9bcf
https://doi.org/10.1016/s1090-3801(09)60437-7
https://doi.org/10.1016/s1090-3801(09)60437-7
Autor:
Stephen J. Medhurst, Sandra Arpino, James Wright, Darren Jason Mitchell, Alexander J. Stevens, James Biggs, Kim Winborn, Susan Marie Westaway, John B. Davis, Jeffrey C. Jerman, Vicky Holland, Tanya Coleman, Jennifer E. Cryan, Geoffrey Stemp, Sarah C. Lappin, Jon T. Seal, Harshad Kantilal Rami, Leontine Saskia Trouw, Mervyn Thompson, Martin J. Gunthorpe
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(20)
6-Phenylnicotinamide (2) was previously identified as a potent TRPV1 antagonist with activity in an in vivo model of inflammatory pain. Optimization of this lead through modification of both the biaryl and heteroaryl components has resulted in the di
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87b365ea545812a5b73fbe175229b22f
https://pubmed.ncbi.nlm.nih.gov/18809327
https://pubmed.ncbi.nlm.nih.gov/18809327
Autor:
Sharon Bingham, Andrew D. Medhurst, Robert G. Dalziel, Iain P. Chessell, Stephen J. Medhurst, Andy Billinton, Jennifer C. Roberts, Amanda Brass, Sue D. Collins
Publikováno v:
PainReferences. 138(1)
Several studies have implicated a potential role for histamine H 3 receptors in pain processing, although the data are somewhat conflicting. In the present study we investigated the effects of the novel potent and highly selective H 3 receptor antago
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::50881dd25935ed7a1bcdab5cda639c75
https://pubmed.ncbi.nlm.nih.gov/18164820
https://pubmed.ncbi.nlm.nih.gov/18164820
Autor:
Nick M. Clayton, Iain P. Chessell, Stephen J. Medhurst, Jon P. Hatcher, Andy Billinton, Sharon Bingham, Christopher J. Hille
Publikováno v:
The journal of pain. 9(7)
The role of specific nicotinic receptor (nAChR) subtypes in antinociception has not been fully elucidated because of the lack, until recently, of selective tool compounds. (R)- N -(1-azabicyclo[2.2.2] oct -3- yl )(5-(2-pyridyl)thiopene-2-carboxamide)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ac37e1d60e6082dc12b2a49d190b23ae
https://pubmed.ncbi.nlm.nih.gov/18420461
https://pubmed.ncbi.nlm.nih.gov/18420461