Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Torquil I. Jack"'
Autor:
Nigel Deeks, Torquil I. Jack, Jonathan D. Goodacre, Martin Sims, Nigel J. Parr, Martin Brandt, Pamela Thomas, Kevin R. Page, Gordon Bruton, James H. Thorpe, Afjal Hussain Miah, Lena Shukla, Duncan S. Holmes, Matthew J Lindon, Leanne Cutler, Erica Christodoulou, David Jonathan Hirst
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:127533
Structure-based led optimisation of orally active reversible Methionine Aminopeptidase-2 (MetAP-2) inhibitors utilising a 'molecular budget' medicinal chemistry strategy is described. The key physicochemical parameters of target molecules (cLogP, mol
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::93cb2e3ab05c206d81698d96ed138dcc
https://doi.org/10.1016/j.bmcl.2020.127533
https://doi.org/10.1016/j.bmcl.2020.127533
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:
S. P. Watson, A.U. Butt, J.M.S. Paton, A.W. Dean, Martin Pass, G.S. Currie, T. Hubbard, M.C. Donnelly, K.S. Cardwell, Torquil I. Jack, David Middlemiss, M.K. Bayliss, N.M. Aston, Duncan B. Judd, Nicola Murdoch Heron, D.G. Allen, T.A. Panchal, A. Hilditch, D. Gallacher, J.E. Hobson, G.M. Drew
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:725-728
The identification of a series of imidazopyridinylbenzofurans (1) as potent, non-peptide antogonists of angiotensin II is described. Several of these compounds cause marked falls in blood pressure in the renal artery ligated rat model of hypertension
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::400a384a545a03eab7bb4d5dd9f3d76a
https://doi.org/10.1016/s0960-894x(01)80188-8
https://doi.org/10.1016/s0960-894x(01)80188-8
Autor:
Martin Pass, M.C. Donnelly, D.I.C. Scopes, Barry Clive Ross, G.R. Manchee, Kenneth L. Clark, T.A. Panchal, A. A. E. Hunt, David Middlemiss, M.K. Bayliss, J.E. Hobson, M.D. Dowle, A. Travers, G.M. Drew, D.G. Walker, Duncan B. Judd, Torquil I. Jack, P.G. Stuart, E. Tranquillini, A. Hilditch, M.J. Robertson, P.J. Eddershaw
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:2047-2050
The identification of GR138950, a non-peptide antagonist of angiotensin II with high oral bioavailability, is described. GR138950 is a potent and selective AT 1 receptor antagonist which causes marked falls in blood pressure in renal hypertensive rat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e99e888e2125cc4f66113c17665aace4
https://doi.org/10.1016/s0960-894x(01)81012-x
https://doi.org/10.1016/s0960-894x(01)81012-x
Autor:
Kenneth Lyle Clark, Steven J Coote, K.S. Cardwell, J.G. Montana, Steve P. Watson, G.C. Hirst, G.R.M. Manchee, J. Hamblett, M.J. Robertson, David Middlemiss, M. Donnelly, B.C. Ross, T.A. Panchal, E. Palmer, J.M.S. Paton, A. Hilditch, G.M. Drew, David I. C. Scopes, M. Pass, M.D. Dowle, J. Bradshaw, Torquil I. Jack, T. Hubbard, M.K. Bayliss, G. Stuart, P. Shah
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:589-594
A study of structure activity relationships based on the bromobenzofuran angiotensin II antagonist GR117289 is reported. This study led to the identification of compounds with potency in vitro enhanced by ca. 10 fold. Also reported is the enhancement
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::dbaea88e6d2f5f5513c4ccd3cdac2b65
https://doi.org/10.1016/s0960-894x(01)81235-x
https://doi.org/10.1016/s0960-894x(01)81235-x
Autor:
Diane M. Coe, David House, Hawa Diallo, Davina C. Angell, Heather A. Barnett, Steve Keeling, Iain M. McLay, Andy Craven, Simon J. F. Macdonald, Tony W. J. Cooper, Torquil I. Jack, Keith Biggadike, Simon Taylor, Samuel Oliver, Iain Uings, James Gray, Natalie Wellaway
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(4)
A novel series of indazole non-steroidal glucocorticoid receptor agonist has been discovered. This series features a sulfonamide central core and meta amides which interact with the extended ligand binding domain. This series has produced some of the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4787d650b1bd623c9d2c0dabec5e4b3
https://pubmed.ncbi.nlm.nih.gov/21257309
https://pubmed.ncbi.nlm.nih.gov/21257309
Autor:
Heather E. Fulton, Torquil I. Jack, Derek N. Evans, Barry A. Coomber, Peter M. Colman, Paul Wyatt, Jose Varghese, Alan J. Wonacott
Publikováno v:
ChemInform. 32
SAR investigations of the 4- and 5-positions of a series of 4-amino-4H-pyran-2-carboxylic acid 6-carboxamides are reported. Potent inhibitors of influenza A sialidase with marked selectivity over the influenza B enzyme were obtained when the basic 4-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0dab81323990861648a74d9c9bd70964
https://doi.org/10.1002/chin.200122144
https://doi.org/10.1002/chin.200122144
Autor:
J Akers, D.I.C. Scopes, M.D. Dowle, Steven John Coote, P. Shah, J Hamblett, C.D. Eldred, Barry Clive Ross, M. J. Robertson, J.M.S. Paton, T.A. Panchal, G.M. Drew, G Stuart, K. L. Clark, A. Hilditch, A. Travers, Torquil I. Jack, K.S. Cardwell, G.C. Hirst, John Gary Montana, David Middlemiss
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 1:711-716
This paper describes the synthesis and pharmacology of a novel series of benzofurans which are antagonists of angiotensin II. One of these, the bromobenzofuran 11b, is a potent (apparent pKB=9.8) and specific antagonist of angiotensin II which, after
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::55219f2de81f8548b7ffa26c3216bf4b
https://doi.org/10.1016/s0960-894x(01)81053-2
https://doi.org/10.1016/s0960-894x(01)81053-2
Autor:
Derek N. Evans, Paul Wyatt, Barry A. Coomber, Alan J. Wonacott, Peter M. Colman, Heather E. Fulton, Torquil I. Jack, Jose Varghese
Publikováno v:
Bioorganicmedicinal chemistry letters. 11(5)
SAR investigations of the 4- and 5-positions of a series of 4-amino-4H-pyran-2-carboxylic acid 6-carboxamides are reported. Potent inhibitors of influenza A sialidase with marked selectivity over the influenza B enzyme were obtained when the basic 4-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::71671076a825c491f2736425abd18073
https://pubmed.ncbi.nlm.nih.gov/11266166
https://pubmed.ncbi.nlm.nih.gov/11266166