Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Colin J. Theobald"'
Autor:
V.Ann Lewis, Ian Stansfield, Kevin J. Milliner, Ivan Leo Pinto, Jackie C. Bloomer, Steven J. Stanway, Stephen A. Smith, Josie A. Blackie, Colin J. Theobald, Beverley Hammond, Hung Yuan Cheng, Colin A. Leach, Maxine A. Taylor, Robert J. Ife, Richard L. Elliott, Deirdre Mary Bernadette Hickey, Murray J. B. Brown, Caroline M. Whittaker, Kitty Moores, Colin H. Macphee
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:2603-2606
The introduction of a functionalised amido substituent into a series of 1-(biphenylmethylacetamido)-pyrimidones has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A(2) with sub-nanomolar potency and very encouraging
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::543d3185255171f3d1d06440ebbf8160
https://doi.org/10.1016/s0960-894x(02)00473-0
https://doi.org/10.1016/s0960-894x(02)00473-0
Autor:
Deirdre M. B. Hickey, Ian Stansfield, Leach Colin Andrew, Caroline M. Whittaker, Ivan Leo Pinto, Stephen A. Smith, Stephen Christopher Martin Fell, Sean Thomas Flynn, Kitty Moores, Helen F. Boyd, Colin J. Theobald, David G. Tew, Roderick A. Porter, Robert John Ife, Kevin J. Milliner, Colin H. Macphee, D. Anthony Rawlings
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2557-2561
From two related series of 2-(alkylthio)-pyrimidones, a novel series of 1-((amidolinked)-alkyl)-pyrimidones has been designed as nanomolar inhibitors of human lipoprotein-associated phopholipase A 2 . These compounds show greatly enhanced activity in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::61b4f0fdf2a2319eb0de05bd3b745d1e
https://doi.org/10.1016/s0960-894x(00)00510-2
https://doi.org/10.1016/s0960-894x(00)00510-2
Autor:
Martin Jones, Colin J. Theobald, Leach Colin Andrew, Sean Thomas Flynn, Deirdre M. B. Hickey, Ian Stansfield, David G. Tew, Brian Peter Slingsby, Helen F. Boyd, Stephen A. Smith, Kevin J. Milliner, Colin H. Macphee, Robert John Ife, D. Anthony Rawlings
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:395-398
Starting from two weakly active hits from high throughput screening, a novel series of 2-(alkylthio)-pyrimidin-4-ones with high potency and selectivity for lipoprotein-associated phospholipase A2 has been designed. In contrast to previously known inh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9832c3ed3c350817610bb873db261f08
https://doi.org/10.1016/s0960-894x(00)00002-0
https://doi.org/10.1016/s0960-894x(00)00002-0
Publikováno v:
Biochemistry. 37:10087-10093
Investigation of the inhibition of LDL-associated phospholipase A2 by monocyclic beta-lactams has shown that LDL phospholipase A2 is capable of hydrolyzing monocyclic-beta-lactams by a mechanism which shares many similarities to the hydrolysis of bet
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f3b58784c3369b656b58cba508ced9b0
https://doi.org/10.1021/bi9801412
https://doi.org/10.1021/bi9801412
Autor:
Leach Colin Andrew, David R. Reavill, Kenneth Wiggall, Colin J. Theobald, David J. Keeling, Robert John Ife, Thomas Henry Brown, Malcolm L. Meeson, Michael E. Parsons
Publikováno v:
Journal of Medicinal Chemistry. 35:3413-3422
Previously, gastric (H+/K+)-ATPase inhibitors such as 2 have been prepared as analogues of 1a on the presumption that the 3-carbethoxy substituent plays a key role in establishing the orientation of the 4-arylamino group. In this paper we explore fur
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::79cebd31e4331d8b5aab573022f2e5ce
https://doi.org/10.1021/jm00096a018
https://doi.org/10.1021/jm00096a018
Autor:
V.Ann Lewis, Colin A. Leach, Colin H. Macphee, Kitty Moores, Murray J. B. Brown, Ivan Leo Pinto, Stephen A. Smith, Robert J. Ife, Ian Stansfield, Steven J. Stanway, Jackie C. Bloomer, Kevin J. Milliner, Maxine A. Taylor, Deirdre Mary Bernadette Hickey, Beverley Hammond, Hung Yuan Cheng, Colin J. Theobald, Josie A. Blackie
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(6)
Modification of the pyrimidone 5-substituent in clinical candidate SB-435495 has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A 2 with sub-nanomolar potency. Cyclopentyl fused derivative 21 , SB-480848, showed an e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2aad2624af5b4abe3cc1d0fa62fcc67e
https://pubmed.ncbi.nlm.nih.gov/12643913
https://pubmed.ncbi.nlm.nih.gov/12643913
Autor:
Josie A, Blackie, Jackie C, Bloomer, Murray J B, Brown, Hung-Yuan, Cheng, Richard L, Elliott, Beverley, Hammond, Deirdre M B, Hickey, Robert J, Ife, Colin A, Leach, V Ann, Lewis, Colin H, Macphee, Kevin J, Milliner, Kitty E, Moores, Ivan L, Pinto, Stephen A, Smith, Ian G, Stansfield, Steven J, Stanway, Maxine A, Taylor, Colin J, Theobald, Caroline M, Whittaker
Publikováno v:
Bioorganicmedicinal chemistry letters. 12(18)
The introduction of a functionalised amido substituent into a series of 1-(biphenylmethylacetamido)-pyrimidones has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A(2) with sub-nanomolar potency and very encouraging
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::9e5ae07f50acb7bdb73023c55e085267
https://pubmed.ncbi.nlm.nih.gov/12182870
https://pubmed.ncbi.nlm.nih.gov/12182870
Autor:
Helen F. Boyd, Stephen Christopher Martin Fell, Stephen A. Smith, Deirdre Mary Bernadette Hickey, Colin A. Leach, Colin J. Theobald, Colin H. Macphee, Caroline M. Whittaker, D. Anthony Rawlings, Ivan Leo Pinto, Ian Stansfield, Steven J. Stanway, Kevin J. Milliner, Robert J. Ife
Publikováno v:
Bioorganicmedicinal chemistry letters. 12(1)
A series of 1-(biphenylmethylamidoalkyl)-pyrimidones has been designed as nanomolar inhibitors of recombinant lipoprotein-associated phospholipase A 2 with high potency in whole human plasma. 5-(Pyrazolylmethyl) derivative 16 and 5-(methoxypyrimidiny
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a88cbaac7c837f62de450e2da3990d3e
https://pubmed.ncbi.nlm.nih.gov/11738571
https://pubmed.ncbi.nlm.nih.gov/11738571
Autor:
Maxine A. Taylor, Robert J. Ife, Colin H. Macphee, Kevin J. Milliner, Ivan Leo Pinto, Jackie C. Bloomer, Steven J. Stanway, Colin A. Leach, D. Anthony Rawlings, Stephen A. Smith, Ian Stansfield, Caroline M. Whittaker, Helen F. Boyd, Colin J. Theobald, Deirdre Mary Bernadette Hickey
Publikováno v:
Bioorganicmedicinal chemistry letters. 11(14)
The lipophilic 1-substituent in a series of 1-((amidolinked)-alkyl)-pyrimidones, inhibitors of recombinant lipoprotein-associated phospholipase A 2 , has been modified to give inhibitors of high potency in human plasma and enhanced physicochemical pr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::056211c5538d978208df8f87cd60c1f3
https://pubmed.ncbi.nlm.nih.gov/11459662
https://pubmed.ncbi.nlm.nih.gov/11459662
Autor:
Colin A. Leach, Colin H. Macphee, V.Ann Lewis, Kevin J. Milliner, Ivan Leo Pinto, Ian Stansfield, Robert J. Ife, Caroline M. Whittaker, Beverley Hammond, Helen F. Boyd, Deirdre Mary Bernadette Hickey, Stephen A. Smith, Colin J. Theobald
Publikováno v:
Bioorganicmedicinal chemistry letters. 11(5)
Modification of the pyrimidone 5-substituent in a series of 1-((amidolinked)-alkyl)-pyrimidones, lipophilic inhibitors of lipoprotein-associated phospholipase A2, has given inhibitors of nanomolar potency and improved physicochemical properties. Comp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::33b9f3a4a8b9227e0e3cf823d002f5ae
https://pubmed.ncbi.nlm.nih.gov/11266173
https://pubmed.ncbi.nlm.nih.gov/11266173