Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Mark Patrick Healy"'
Autor:
Tarik Khaznadar, Helen Susanne Price, Andy Billinton, Martin E. Swarbrick, David Andrew Stevens, Gerard Martin Paul Giblin, Melanie A. Kay, Anton D. Michel, Nicholas Maughan Clayton, David J. Spalding, Alan Naylor, Alex W. Wilson, Amanda C. Allan, Mark Patrick Healy, Iain P. Chessell, Kristin Bailey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:1892-1896
A novel series of EP4 agonists and antagonists have been identified, and then used to validate their potential in the treatment of inflammatory pain. This paper describes these novel ligands and their activity within a number of pre-clinical models o
Publikováno v:
Catal. Sci. Technol.. 4:3524-3533
Gold(III) catalysts mediate 1,5-enyne cycloisomerization or tandem nucleophilic substitution-1,5-enyne cycloisomerization processes in an efficient manner. This study examines the reaction kinetics of 1,5-enyne cycloisomerization, mediated by AuBr2(N
Publikováno v:
Organometallics. 32:3108-3120
The effects of substituting (pseudo)halide for anionic imidate ligands in Au(I) and Au(III) (i.e. [AuBr(NHC)] and [AuBr3(NHC)]) complexes have been investigated. [Au(N-imidate)(NHC)] and [AuBr2(N-imidate)(NHC)] complexes were prepared and the structu
Autor:
Stephen John Atkinson, Gerard Martin Paul Giblin, Paul Goldsmith, Anton D. Michel, Anita Chowdhury, Mark Patrick Healy, Karamjit S. Jandu, Jennifer Sweeting, Matthew R. Johnson, Iain P. Chessell, Adrian Hall, Alan Naylor, Susan H. Brown
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1200-1205
Replacement of the carboxylic acid group in a series of previously described 1,5-biaryl pyrrole EP 1 receptor antagonists led to the discovery of various novel non-acidic antagonists. Several analogues displayed high binding affinity and high binding
Autor:
Matthew R. Johnson, Adrian Hall, Stephen P. Watson, Stephen C. McKeown, Alan Naylor, Iain P. Chessell, Anita Chowdhury, Richard J. Wilson, Xiao Qing Lewell, Susan H. Brown, Gerard Martin Paul Giblin, Mark Patrick Healy, Olivier Lorthioir, Richard Blunt, Anton D. Michel, Wendy J. Winchester, Shilina Roman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1750-1754
A high-throughput screen targeting the EP1 receptor identified non-acidic glycine sulfonamide derivative 2a with a pKi of 6.2. Analogue synthesis allowed a thorough investigation of the structure–activity relationship (SAR) and led to a 100-fold in
Autor:
Gerard Martin Paul Giblin, Anton D. Michel, Adrian Hall, Riccardo Novelli, Matthew R. Johnson, Alan Naylor, Susan H. Brown, David J. Spalding, Nicholas Maughan Clayton, Mark Patrick Healy, Anita Chowdhury, Jennifer Sweeting, Iain P. Chessell, Tanya Coleman, Beverley Hammond, Ann Metcalf
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:732-735
This paper details the SAR of 1,5-biaryl pyrrole derivatives with substituents in the 2-, 4-, and 5-positions of the benzoic acid group as EP1 receptor antagonists. Substitution at the 2-position was poorly tolerated, whereas only fluorine was tolera
Autor:
Anne F. Kornahrens, Darren L. Poole, Di Shen, Timothy J. Donohoe, Camilla C. Shotton, Mark Patrick Healy
Publikováno v:
ChemInform. 46
[IrCl(cod)]2 as the catalyst promotes hydrogen-borrowing reaction of ketone enolates with methanol to give enones (III) which can react with excess methanol as nucleophile to yield mixtures of methoxymethyl derivatives (IV) and the enones (III).
Autor:
Anne F. Kornahrens, Di Shen, Camilla C. Shotton, Mark Patrick Healy, Timothy J. Donohoe, Darren L. Poole
Publikováno v:
Angewandte Chemie (International Ed. in English)
Reported herein is the use of catalytic [{Ir(cod)Cl}2 ] to facilitate hydrogen-borrowing reactions of ketone enolates with methanol at 65 °C. An oxygen atmosphere accelerates the process, and when combined with the use of a bulky monodentate phosphi
Autor:
Nicholas Maughan Clayton, Gerard Martin Paul Giblin, Mark Patrick Healy, Anton D. Michel, Riccardo Novelli, Beverley Hammond, Stephen John Atkinson, Sac P. Tang, Susan H. Brown, Matthew R. Johnson, Anita Chowdhury, Alan Naylor, David J. Spalding, Adrian Hall, Iain P. Chessell, Robert Gleave, Tanya Coleman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:3657-3662
The preliminary SAR of a series of novel 1,5-biaryl pyrrole EP1 receptor antagonists derived from compound 1 is described. Replacement of the benzyl group of 1 with isosteric groups was investigated. The most effective replacement was found to be the
Publikováno v:
ChemInform. 41
(ItPe)AuBr2(N-imidate) complexes, prepared in high yield by oxidative bromination, are active catalysts for 1,5-enyne cycloisomerization. An efficient tandem nucleophilic substitution–1,5-enyne cycloisomerization is promoted by these novel Au(III)