Zobrazeno 1 - 10
of 52
pro vyhledávání: '"Nigel S. Watson"'
Autor:
Stefan Senger, Máire A. Convery, Robert J. Young, Stephanie Irvine, Iain M. McLay, Robert I. West, David J. Belton, Savvas Kleanthous, Carl Adams, John R. Toomey, Anne M. Exall, Anthony J. Pateman, Theresa J. Roethke, Caroline M. Whittaker, Laiq Chaudry, David E. Davies, Angela Patikis, Cynthia L. Burns-Kurtis, Nigel S. Watson, Gary J. Stelman, David W. Brown, John D. Harling, Wendy R. Irving, Chuen Chan, Ping Zhou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1588-1592
The discovery and evaluation of potent and long-acting oral sulfonamidopyrrolidin-2-one factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs are described. Unexpected selectivity issues versus tissue plasminogen activator in the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dff85f937ce4e89e1a2bcffaac9ddca4
https://doi.org/10.1016/j.bmcl.2011.01.129
https://doi.org/10.1016/j.bmcl.2011.01.129
Autor:
Anthony J. Pateman, John R. Toomey, Paul F. Koster, Augustin Amour, Saul Needle, Laiq Chaudry, Melanie A Abboud, Champa Patel, Angela Patikis, Cynthia L. Burns-Kurtis, Robert J. Young, Richard E. Valocik, David Brown, Ping Zhou, Chuen Chan, Nigel S. Watson
Publikováno v:
Journal of Cardiovascular Pharmacology. 52:66-71
Background: Factor Xa (FXa) has been a target of considerable interest for drug development efforts aimed at suppressing thrombosis. In this report, a new orally active, small molecule, active-site directed FXa inhibitor, GW813893, has been profiled
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e4ecf88e87e341213f5fef72bbcb248
https://doi.org/10.1097/fjc.0b013e31817e9b9e
https://doi.org/10.1097/fjc.0b013e31817e9b9e
Autor:
Alan D. Borthwick, Marie Charbaut, Robert J. Young, Máire A. Convery, Ivan Leo Pinto, Andrew M. Mason, Weston Helen Elisabeth, Matthew Campbell, David W. Brown, Anthony J. Pateman, Henry Anderson Kelly, Derek Pollard, Shah Gita Punjabhai, John R. Toomey, N. Paul King, Stefan Senger, Eric Hortense, Ping Zhou, Hawa Diallo, Nigel S. Watson, Wendy R. Irving, Angela Patikis, Cynthia L. Burns-Kurtis, Savvas Kleanthous, Chuen Chan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:28-33
Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating basic biaryl P4 groups, producing highly potent inhibitors with significant anticoagulant activitie
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03145f782eb525e093f927857c7919cd
https://doi.org/10.1016/j.bmcl.2007.11.019
https://doi.org/10.1016/j.bmcl.2007.11.019
Autor:
Robert J. Young, David W. Brown, Stefan Senger, Chuen Chan, Máire A. Convery, Anthony J. Pateman, Nigel S. Watson, John R. Toomey, Ping Zhou, Henry Anderson Kelly, Shah Gita Punjabhai, Julia A. Hubbard, Angela Patikis, Cynthia L. Burns-Kurtis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2927-2930
The synthetic entry to new classes of dual fXa/thrombin and selective thrombin inhibitors with significant oral bioavailability is described. This was achieved through minor modifications to the sulfonamide group in our potent and selective fXa inhib
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::29c69eec9dfca70c859103d7b56e8c3a
https://doi.org/10.1016/j.bmcl.2007.03.080
https://doi.org/10.1016/j.bmcl.2007.03.080
Autor:
Nicolas Morley, Deborah Wild, Peter J Sharratt, Nigel S. Watson, Panayiotis Alexandrou Procopiou, Brian Cox
Publikováno v:
Tetrahedron Letters. 41:7547-7550
Squalestatin 3,4-β-lactone-4,5-dimethyl ester (8) was reductively ring-opened to yield squalestatin 3-hydroxymethyl-4,5-dimethyl ester (6) using mild reducing conditions (sodium borohydride). Similarly, squalestatin 3,4-oxetane-4,5-dimethyl ester (1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::db5f1d515f21e9c891d9cd2c1c8f653f
https://doi.org/10.1016/s0040-4039(00)01286-7
https://doi.org/10.1016/s0040-4039(00)01286-7
Autor:
Philip J. Sidebottom, Panayiotis A. Procopiou, Brian Dymock, Stephen J. Spooner, Graham G. A. Inglis, Anton R. P. Srikantha, Andrew D. Roberts, Michael George Lester, Nigel S. Watson
Publikováno v:
Journal of the Chemical Society, Perkin Transactions 1. :327-334
Reaction of 2 with Ac2O–TMSOTf gives the triacetate 5, which on further reaction gives isomer 6, arising from an allylic rearrangement, whereas reaction of 2 with Et3SiH–TMSOTf gives tricycle 7 arising from addition of the C7-OH to the allylic ce
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1fc88f1f9d1d7eb00a3fe0703fc23827
https://doi.org/10.1039/a704363e
https://doi.org/10.1039/a704363e
Publikováno v:
Tetrahedron Letters. 37:8925-8928
Synthesis of squalcstalin S1 C-4 carboxamide, 2, as well as related C-4 amides and C-4 hydroxymethyl derivatives possessing a C-3 hydroxymethyl group (15 and 19) together with their SQS inhibitory activities arc presented.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::dcfe69aa96cbc61b793cc3f79c2d570c
https://doi.org/10.1016/s0040-4039(96)02049-7
https://doi.org/10.1016/s0040-4039(96)02049-7
Autor:
Daniele Andreotti, Nigel S. Watson, Meenu Sareen, Chuen Chan, Jan Josef Scicinski, Alun D McCarthy, Panayiotis Alexandrou Procopiou, Brian Dymock, B.C. Ross, Michael A. Snowden, Keeling Suzanne Elaine, Julie L. Hutson, Brian Cox, Peter J Sharratt
Publikováno v:
Journal of Medicinal Chemistry. 39:207-216
Squalestatins without either the hydroxy group at C-4 or the carboxylic acid at C-3 or C-4 were prepared and evaluated for their ability to inhibit rat liver microsomal squalene synthase (SQS) in vitro. These modifications were well tolerated for com
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a401dd488a7564884a3acf803da730cf
https://doi.org/10.1021/jm9504969
https://doi.org/10.1021/jm9504969
Autor:
Meenu Sareen, Panayiotis A. Procopiou, Anton A.P. Srikantha, Nigel S. Watson, Michael G. Lester, Richard A. Henson, Stephen J. Spooner, Michael A. Snowden, Gary L. Evans
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:2683-2688
The C4′ acetoxy group in squalestatin 2a has been replaced by alkoxy, acyloxy and acetamido groups. The ethers 5b, 5c, 5e and 5g retain SQS inhibitory activity equivalent to that of 2a and are metabolically more stable. All other compounds tested a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::15b06a102230b6718f32c0e144eceead
https://doi.org/10.1016/s0960-894x(01)80696-x
https://doi.org/10.1016/s0960-894x(01)80696-x
Autor:
B. E. Kirk, Nigel S. Watson, Anton R. P. Srikantha, Julie L. Hutson, Brian Cox, Keeling Suzanne Elaine
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:1931-1936
A series of 3-hydroxymethyl derivatives of squalestatin 1 was prepared as inhibitors of squalene synthase. Potent in vitro inhibitory activity is retained in those analogues which possess C-6 and C-1 substituents analogous to those found in 1.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::cf22bcd2a21a45efc943f712abee7f42
https://doi.org/10.1016/s0960-894x(01)80537-0
https://doi.org/10.1016/s0960-894x(01)80537-0