Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Leach Colin Andrew"'
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
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
Autor:
Helen F. Boyd, Deirdre M. B. Hickey, Kitty Moores, Kevin J. Milliner, Colin H. Macphee, Dash Dhanak, Keith E. Suckling, Leach Colin Andrew, Rebecca A. Patterson, Robert John Ife, David S. Leake, David G. Tew
Publikováno v:
Biochemical Journal. 338:479-487
A novel and potent azetidinone inhibitor of the lipoprotein-associated phospholipase A2 (Lp-PLA2), i.e. platelet-activating factor acetylhydrolase, is described for the first time. This inhibitor, SB-222657 (Ki = 40±3 nM, kobs/[I] = 6.6×105 M-1·s-
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
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:543-546
4-(2-Pyridyl)-5-phenylthiazoles, 3 (X = S), are shown to be reversible, K + -competitive gastric H + /K + -ATPase inhibitors. It is suggested that a hydrogen-bond between the protonated pyridine and the thiazole may help the molecule adopt a conforma
Autor:
David J. Keeling, M. E. Parsons, Robert John Ife, S. M. Laing, C. A. Price, K. J. Wiggall, Leach Colin Andrew, T. H. Brown
Publikováno v:
ChemInform. 24
Autor:
Leach Colin Andrew, David G. Tew, Deirdre M. B. Hickey, Stephen A. Smith, Robert John Ife, Colin H. Macphee
Publikováno v:
ChemInform. 32
Lipoprotein-associated phospholipase A2 (Lp-PLA2) is a serine lipase that is associated with low density lipoprotein (LDL) in human plasma. Substrates include oxidised phosphatidylcholine (PC), which is hydrolysed by Lp-PLA2 to lyso-PC and oxidised f
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
Autor:
Michael E. Parsons, Leach Colin Andrew, Kenneth Wiggall, David J. Keeling, Thomas Henry Brown, Carolyn A. Price, Shiona M. Laing, Robert John Ife
Publikováno v:
Journal of Medicinal Chemistry. 35:1845-1852
Further work on compounds 1 has identified the 4-position as a site where substantial modifications are tolerated, leading to analogues which are more potent and less toxic than those described previously. The best compound in the series is 13a (SK&F
Autor:
Leach Colin Andrew, David J. Keeling, Colin J. Theobald, Malcolm L. Meeson, Robert John Ife, Michael E. Parsons, Peter Blurton, Thomas Henry Brown
Publikováno v:
Journal of medicinal chemistry. 38(14)
Quinazolines bearing a secondary 4-(arylamino) substituent demonstrate an SAR for inhibition of the gastric (H + /K + )-ATPase different from the previously described 3-acylquinolines, suggesting that, although these compounds are also K + -competiti