Zobrazeno 1 - 10
of 44
pro vyhledávání: '"Gordon A. Weingarten"'
Autor:
Philip Alan Skone, Donald O. Somers, Marion C. Dickson, Nick Smithers, Ann Louise Walker, Thomas George Christopher Hayhow, Stuart G. Leach, Karen Leavens, Clement Douault, Emma J. Jones, Dorothy Elwes, Robert J. Watson, Margarete Neu, Robert P. Davis, Matthew Gray, Neil Stuart Garton, Clare I. Hobbs, Alex Preston, Michael David Barker, Vipulkumar Kantibhai Patel, Cesar Ramirez-Molina, Paul S. Carter, Scott McCleary, Gordon G. Weingarten, Huw D. Lewis, Francis Louis Atkinson, John Liddle, Tracy Jane Shipley, Neil R. Curtis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6188-6194
The lead optimisation of the diaminopyrimidine carboxamide series of spleen tyrosine kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient margin over l
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58fce9afb90ca4e724d4726df2268b6f
https://doi.org/10.1016/j.bmcl.2011.07.082
https://doi.org/10.1016/j.bmcl.2011.07.082
Autor:
Isabel Casades, M. Joseph Colston, Helen C. Hailes, Kerry J. Goodworth, Alison M. Hill, Ricardo E. Tascon, Gordon G. Weingarten, Gwenaelle Hervé, Anne-Cécile Hervé, Evangelos Stavropoulos
Publikováno v:
Tetrahedron. 67:373-382
A series of large-ringed calix[6,7,8]arene analogues have been synthesised and their affect against Mycobacterium tuberculosis in vivo established. In general, when p-phenylcalixarenes and tert-butylcalixarenes were not functionalised at the lower ri
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c88d73917a5e7939ccadd81397e18f90
https://doi.org/10.1016/j.tet.2010.11.034
https://doi.org/10.1016/j.tet.2010.11.034
Autor:
Amanda J. Campbell, Stephen P. Marsden, Adam Nelson, Rachel J. Shearer, David House, Joachim Horn, Ho Yin Li, Gordon G. Weingarten
Publikováno v:
Tetrahedron. 65:9002-9007
An efficient and convergent one-step synthesis of substituted dihydroquinolin-2-ones from α,β-unsaturated esters and aminoaryl pinacolboronates under rhodium catalysis is reported. The reaction is easily applicable in parallel synthesis format and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0cd0baa2eeddfd49d0809bf3ddd71beb
https://doi.org/10.1016/j.tet.2009.06.103
https://doi.org/10.1016/j.tet.2009.06.103
Autor:
Simon J. F. Macdonald, Graham I. Somers, Natalie Rayner, Tony W. J. Cooper, Iain Mcfarlane Mclay, James Michael Woolven, Simon Taylor, Rosemary Z. Sasse, Gordon G. Weingarten, Diane Mary Coe, Heather A. Barnett, Tracy Jane Shipley, Iain Uings, Phil A. Skone, Torquil I. Jack, Haydn Terence Jones
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:158-162
Aryl aminopyrazole amides capped with N-alkylbenzamides 13-16 are selective glucocorticoid receptor agonists. 2,6-Disubstituted benzamides have prednisolone-like potency or better in vitro. Good oral exposure was demonstrated in the rat, with compoun
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::401ca21d58e44b527a101830a268de32
https://doi.org/10.1016/j.bmcl.2008.10.128
https://doi.org/10.1016/j.bmcl.2008.10.128
Autor:
Simon J. F. Macdonald, Philip Alan Skone, Ian B. Campbell, Diane M. Coe, Tony W. J. Cooper, Gordon A. Weingarten, Peter W. Sutton, Deborah Needham, George Hardy, Tracy Jane Shipley, Haydn Terence Jones, Torquil I. Jack, Steven Philip Keeling
Publikováno v:
Tetrahedron Letters. 49:5101-5104
The efficient synthesis of an α-trifluoromethyl-α-tosyloxymethyl epoxide is reported. This highly versatile building block may be reacted sequentially with two different nucleophiles to furnish α-trifluoromethyl tertiary alcohols. Furthermore, the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::39e5ddf37cef54e5d27b966049701f90
https://doi.org/10.1016/j.tetlet.2008.06.011
https://doi.org/10.1016/j.tetlet.2008.06.011
Autor:
Deborah L. Jackson, Graham J Hart, Angela Patikis, Gordon G. Weingarten, Nigel R. Parry, Alan D. Borthwick, James Michael Woolven, Terry M. Haley, Dave E. Davies, Anne M. Exall, Peter Franz Ertl, Naimisha Trivedi
Publikováno v:
Journal of Medicinal Chemistry. 46:4428-4449
A series of chiral, (S)-proline-alpha-methylpyrrolidine-5,5-trans-lactam serine protease inhibitors has been developed as antivirals of human cytomegalovirus (HCMV). The SAR of the functionality on the proline nitrogen has shown that derivatives of p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c2b6a73dae4a667f9c1ac9169b95e88
https://doi.org/10.1021/jm030810w
https://doi.org/10.1021/jm030810w
Autor:
Fabrizio Nerozzi, Shalia S Shabbir, Paul G. Wyatt, Mamta Patel, Michael Allen, Josie Chilcott, Christopher J. Gardner, Marion J. Perren, Jackie E. Mordaunt, Livermore David, Gordon G. Weingarten, Ping Zhou, Patrick M. Woollard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1405-1411
The paper covers continuing efforts to discover novel, potent and selective oxytocin antagonists. Further benzofuran derivatives with potent oxytocin antagonist activity and good pharmacokinetic parameters are reported. Efforts to improve the in vivo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e1b65e9e762608b3da232e63c0d7e45
https://doi.org/10.1016/s0960-894x(02)00160-9
https://doi.org/10.1016/s0960-894x(02)00160-9
Autor:
Gordon G. Weingarten, and Andrew M. K. Pennell, Andrew Mcmurtrie Mason, Andrew James Crame, Terry M. Haley, Graham J. Hart, Anne M. Exall, S. Jane Angier, Alan D. Borthwick
Publikováno v:
Journal of Medicinal Chemistry. 43:4452-4464
Mechanism-based inhibitors of human cytomegalovirus (HCMV) protease have been designed based on the pyrrolidine-5,5-trans-lactam ring system. New routes to the beta-methyl-, desmethyl-, and alpha-methyl-pyrrolidine-5,5-trans-lactam templates have bee
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c79032edf1c97470d3605c9cb4172955
https://doi.org/10.1021/jm000078q
https://doi.org/10.1021/jm000078q
Publikováno v:
Journal of the Chemical Society, Perkin Transactions 1. :3469-3476
Overall 5-endo-trig iodocyclisations of all isomers of the 2-alkenylcyclopentan-1-ols and -cyclohexan-1-ols 11, 12, 14 and 16 have been examined. Only in the cases of the trans-alkenylcyclopentanols 11a and 12a are the reactions either unsuccessful o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4f65e73aaa870300645986a560524d94
https://doi.org/10.1039/b004684l
https://doi.org/10.1039/b004684l
Autor:
Alan D. Borthwick, Haloun Jin, Leonard Yuen, Tarek S. Mansour, Gordon G. Weingarten, Mirek Tomaszewski, Jean Bedard, Zhouhan Hu, Terry M. Haley, Wei Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:365-370
Mechanism based inhibitors of HCMV protease have been designed based on the monocyclic beta-lactam nucleus, which have been shown to acylate the viral enzyme in a time dependent manner. SAR in a series of monocyclic beta-lactam N-ureas, has defined t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::622a643a453be69d4e112d9b316a78ef
https://doi.org/10.1016/s0960-894x(98)00032-8
https://doi.org/10.1016/s0960-894x(98)00032-8