Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Michael Paradowski"'
Neurosteroid Modulation of Synaptic and Extrasynaptic GABAA Receptors of the Mouse Nucleus Accumbens
Autor:
Scott J. Mitchell, Grant D. Phillips, Becks Tench, Yunkai Li, Delia Belelli, Stephen J. Martin, Jerome D. Swinny, Louise Kelly, John R. Atack, Michael Paradowski, Jeremy J. Lambert
Publikováno v:
Biomolecules, Vol 14, Iss 4, p 460 (2024)
The recent approval of formulations of the endogenous neurosteroid allopregnanolone (brexanolone) and the synthetic neuroactive steroid SAGE-217 (zuranolone) to treat postpartum depression (PPD) has encouraged further research to elucidate why these
Externí odkaz:
https://doaj.org/article/e9f4ea689ff047bdb0ce891c119b69a6
Autor:
Richard M. Angell, John Ludes-Meyers, Simon E. Ward, Michael Paradowski, Irina Chuckowree, Alexandre Bedernjak, James Lumley, Carol Villalonga Barber, Kenneth Powell, Edward Littler, Daniel Watterson, Geraldine Taylor, Elaine Thomas, Jose Gascon-Simorte, Mark E. Peeples, Michelle Thom, Jason S. McLellan, Dereck Tait, Neil Mathews, Paul R. Young, Ian M. Fraser, Morgan S.A. Gilman, James A. D. Good, G. Stuart Cockerill, Rachel Harland, Sara M. Johnson, Graham Lunn, Claire Scott, Gareth Williams
RV521 is an orally bioavailable inhibitor of respiratory syncytial virus (RSV) fusion that was identified after a lead optimization process based upon hits that originated from a physical property directed hit profiling exercise at Reviral. This exer
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8371da7b3d3bd17095117d7ce4913054
https://orca.cardiff.ac.uk/id/eprint/143067/1/jm-2020-01882r.R2_Proof_hi.pdf
https://orca.cardiff.ac.uk/id/eprint/143067/1/jm-2020-01882r.R2_Proof_hi.pdf
Autor:
Paul John Beswick, Mark A. Honey, Ruth D. Murrell-Lagnado, Ben Wahab, Martin Lochner, Michael Paradowski, Ke Jiang, Andrew J. Thompson
Publikováno v:
Neuropharmacology. 157
Identifying novel small-molecule P2X1 and P2X4 ligands with sub-type specificity and high-affinity remains a pharmacological challenge. Here we use computational methods, electrophysiology and fluorescent microplate assays to screen for ligand candid
Autor:
Michael Paradowski, Srinivasa P. S. Rao, Paul John Beswick, Gareth Williams, Jamie Laverick, Trevor Askwith, John R. Atack, Oran G. O'Doherty, Ryan West, Lewis E. Pennicott, Simon E. Ward
Publikováno v:
European Journal of Medicinal Chemistry
African trypanosomiasis is a parasitic disease affecting 5000 humans and millions of livestock animals in sub-Saharan Africa every year. Current treatments are limited, difficult to administer and often toxic causing long term injury or death in many
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df9413fffece5e2c33062580b7420cc0
http://sro.sussex.ac.uk/id/eprint/71807/1/__smbhome.uscs.susx.ac.uk_lep20_Desktop_1-s2.0-S022352341730781X-main.pdf
http://sro.sussex.ac.uk/id/eprint/71807/1/__smbhome.uscs.susx.ac.uk_lep20_Desktop_1-s2.0-S022352341730781X-main.pdf
Autor:
Kathy F. K. Cheung, Jean-Yves Chiva, Satish Dayal, Darren Stead, Carly L. Nichols, Rob Webster, Lee R. Roberts, David Stonehouse, Felice Daverio, Iain Gardner, Andrew Pike, Michael Paradowski, David C. Blakemore, Gilles H. Goetz, Lesa Watson, Chris Pickford, Jared B.J. Milbank, Ye Che, Robert Wybrow, Florian Wakenhut, Keith Statham, Caroline Smith-Burchnell, Samuel Crook, Fiona M. Adam, David C. Pryde, David Leese, Mike Westby, Duncan Hay, Stephen M. Shaw, Tram T. Tran
Publikováno v:
ChemMedChem. 9:1378-1386
Nonstructural protein 5A (NS5A) represents a novel target for the treatment of hepatitis C virus (HCV). Daclatasvir, recently reported by Bristol-Myers-Squibb, is a potent NS5A inhibitor currently under investigation in phase 3 clinical trials. While
Publikováno v:
Organicbiomolecular chemistry. 14(12)
A novel approach of the convergent functionalisation of aryl dibromides to form NS5A type inhibitors using C–H activation is reported. The focus of investigation was to reduce the formation of homodimeric side product, as well as to investigate the
Autor:
David Howard Williams, Nigel Alan Swain, Charlotte Alice Louise Lane, Michael Paradowski, Duncan Hay, Matthew D. Selby, Charles E. Mowbray
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1156-1159
This letter describes the discovery and synthesis of a series of octahydropyrrolo[3,4-c]pyrrole based selective histamine hH4 receptor antagonists. The amidine compound 20 was found to be a potent and selective histamine H4 receptor antagonist with m
Publikováno v:
Tetrahedron. 67:9700-9707
The synthesis of the C1–C16 framework of the ajudazols has been achieved taking advantage of a highly selective isobenzofuran oxidative rearrangement and a key Stille coupling to introduce the key C14–C15 bond.
Autor:
Tram T. Tran, Rachel Dixon, Duncan Hay, James Hitchin, Gemma C. Parsons, David C. Pryde, Gerwyn Bish, Michael Paradowski, Fiona M. Adam, Nicholas Smith, Peter Jones, M. Jonathan Fray, Katie J. W. Proctor, Frederick Calo
Publikováno v:
Tetrahedron Letters. 52:5728-5732
A flexible route which enables access to derivatives of 4-amino-1,3-dihydroimidazo[4,5-c]pyridin-2-ones is described. Issues of selectivity, reaction safety, and low yields in original routes are overcome with the key improvements to the route, inclu
Publikováno v:
Synlett. 2011:1543-1546
A concise synthesis of fused bicyclic pyrrolidines via 1,3-dipolar cycloaddition of azomethine ylides is reported. The exo cycloadduct isomer enables the synthesis of a novel cyclic amidine toward the preparation of a potential human histamine H4 rec