Zobrazeno 1 - 10
of 62
pro vyhledávání: '"Daryl S. Walter"'
Autor:
Simon E. Ward, Jonathan M. Elkins, Daryl S. Walter, Roberta Regina Ruela de Sousa, P.H.C. Godoi, Oleg Fedorov, Scott H. Henderson, Jim Bennett, Sean W. Robinson, Iva Navratilova, Marcus T. Hanley, Alexander Ashall-Kelly, Fiona J. Sorrell
Publikováno v:
Journal of Medicinal Chemistry
Dual-specificity tyrosine-regulated kinase 1A (DYRK1A) regulates the proliferation and differentiation of neuronal progenitor cells during brain development. Consequently, DYRK1A has attracted interest as a target for the treatment of neurodegenerati
Autor:
Thomas M. Zollner, Antonius Ter Laak, Daryl S. Walter, Jens Nagel, Anne-Marie Coelho, Horst Irlbacher, Michaele Peters, Andrea Rotgeri, Marcus Koppitz, Andreas Steinmeyer, Nico Bräuer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:2700-2705
Here we report on novel and potent pyridyl-cycloalkyl-carboxylic acid inhibitors of microsomal prostaglandin E synthase-1 (PTGES). PTGES produces, as part of the prostaglandin pathway, prostaglandin E2 which is a well-known driver for pain and inflam
Autor:
Michael J. Tucker, Timothy J. Donohoe, Ahria Esphandiar Roushanbakhti, Wasim M. Akhtar, Yifan Liu, Daryl S. Walter, Gail L. Wrigley, Paul C. M. Winship
Publikováno v:
Angewandte Chemie International Edition. 56:14883-14887
Catalytic oxidative cyclisation reactions have been employed for the synthesis of the E and F rings of the complex natural product target pectenotoxin 4. The choice of metal catalyst (cobalt- or osmium-based) allowed for the formation of THF rings wi
Autor:
Stefan Bäurle, Olaf Peters, Gernot Langer, Ludwig Zorn, Antonius Ter Laak, Nico Bräuer, Ulrich Bothe, Daryl S. Walter, Jens Nagel, Thomas M. Zollner, Thorsten Blume, Cornelia Preusse, Antje Rottmann, Andreas Steinmeyer, Dieter Heldmann
Publikováno v:
Journal of medicinal chemistry. 62(5)
The presence and growth of endometrial tissue outside the uterine cavity in endometriosis patients are primarily driven by hormone-dependent and inflammatory processes-the latter being frequently associated with severe, acute, and chronic pelvic pain
Autor:
Thelma R. Cowley, Niamh Murphy, Daryl S. Walter, Marina A. Lynch, David Virley, Neil Upton, Jill C. Richardson
Publikováno v:
Brain Pathology. 22:295-306
Release of interleukin (IL)-1β from immunocompetent cells requires formation of the NACHT, LLR and PYD domains-containing protein 3 (NLRP3) inflammasome and caspase 1 activation. Adenosine 5'-triphosphate (ATP), acting on the P2X(7) receptor, is one
Publikováno v:
Chemistry - An Asian Journal. 6:3214-3222
A new strategy that employs an exocyclic stereocenter to effect diastereocontrol in the tethered aminohydroxylation (TA) reaction is applied to the stereoselective synthesis of a range of amino alcohols in good to excellent yields, and with anti sele
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
Autor:
Alan Naylor, Emmanuel Hubert Demont, P. Theobald, Daryl S. Walter, G. Maile, Gareth Wayne, Ishrut Hussain, Colin Dingwall, B. Clarke, C. Howes, Sharon Sweitzer, D. Vesey, Leanne Cutler, Julie Hawkins, Rosalie Matico, J. Mosley, A. O'Brien, Virginie Soleil, Sally Redshaw, Kathrine J. Smith, Paul Rowland, R. Dunsdon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4639-4644
Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer's disease. Herein, is described a series of potent inhibitors based on an hydroxyethylamine (HEA) transition state mimetic template. The
Autor:
Sac-Pham Tang, Robert Gleave, Paul John Beswick, Anton D. Michel, Shilina Roman, Daryl S. Walter, Elena Fonfria
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4951-4954
A series of analogues of the pyrazole lead 1 were synthesized in which the heterocyclic core was replaced with an imidazole. A number of potent antagonists were identified and structure-activity relationships (SAR) were investigated both with respect
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