Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Ronald Palin"'
Publikováno v:
Tetrahedron. 64:3119-3126
The asymmetric synthesis of the potent selective NOP agonist 2-(3-{1-[3-(5-methoxy-2-methyl-phenoxy)-4-methyl-pentyl]-piperidin-4-yl}-2-oxo-2,3-dihydro-benzimidazol-1-yl)-N-methyl-acetamide and analogues was developed. The key step, chiral reduction
Publikováno v:
Anesthesia & Analgesia. 104:174-179
Agonists at the opioid receptor-like receptor 1 (ORL1) induce motor impairment, sedation, and loss of righting reflex (LRR) in rodents. This receptor may provide a novel target in the field of anesthesia.We examined the hypnotic, electroencephalograp
Autor:
Ronald Palin, Hardy Sundaram, Philip S. Jones, David Vrolijk, Louise Evans, Mark A. Weston, David R. Barn, Grove Simon James Anthony, Helen Feilden, John K. Clark, J. Cottney, Marc Crockatt, Alasdair R.C. Smith, Grant Wishart, Paul Wren, Phillip M. Cowley, Richard Morphy, Frank Griekspoor, Richard R. Goodwin, Andrea K. Houghton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:589-593
A series of 3-phenoxypropyl piperidine analogues have been discovered as novel ORL1 receptor agonists. Structure-activity relationships have been explored around the 3-phenoxypropyl region with several potent and selective analogues identified.
Publikováno v:
Magnetic Resonance in Chemistry. 43:647-653
The solution-state NMR spectra of a per-6-substituted γ-cyclodextrin show some interesting dynamic properties. At high temperature (353 K), the 1H NMR spectrum shows dynamic averaging of the different conformations. This averaging is no longer obser
Publikováno v:
Tetrahedron Letters. 42:8897-8899
A reaction between γ-cyclodextrin (γ-CD) and 2,4,6-triisopropylbenzenesulfonyl chloride in pyridine gave mono-6-( O -2,4,6-triisopropylbenzenesulfonyl)-γ-cyclodextrin in good yield (∼69%) and high purity (>98%). In contrast to other sulfonylatio
Autor:
Michael Ohlmeyer, Yajing Rong, Katy Everett, Robert Swanson, Nasrin Ansari, Duncan McArthur, Kenneth S. Cameron, Quynhchi Pham, Irina Neagu, Heather Tracey, Darren Edwards, John Maclean, Maureen Dempster, Thomas R. Clarkson, Hazel McLuskey, Koc-Kan Ho, Helen Feilden, Paul Ratcliffe, David A. Dunn, Andrew Laird Roughton, S.A. Neale, Steve Kultgen, Glenn Walker, Littlewood Peter Thomas Albert, Melanie Sammons, Ronald Palin, Lynn Abernethy, Anna-Marie Easson, Deborah McGregor, Lesley-Anne Nisbet
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(3)
Optimisation of a screening hit incorporating both TRPV1 activity and solubility was conducted. Substitution of the isoxazole-3-carboxamide with the bespoke 1S, 3R-3-aminocyclohexanol motif afforded the requisite balance of potency and solubility. Co
Publikováno v:
ChemInform. 33
Autor:
Duncan McArthur, Alasdair R.C. Smith, Niall M. Hamilton, Louise Evans, Ronald Palin, Helen Feilden, Dan Fletcher, Grant Wishart, Aaron Sutherland, Philip S. Jones, Mark A. Weston, Paul Ratcliffe, John K. Clark, Brian Montgomery, Andrea K. Houghton
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(22)
A knowledge based approach has been adopted to identify novel NOP receptor agonists with simplified hydrophobes. Substitution of the benzimidazol-2-one piperidine motif with a range of hydrophobic groups and pharmacophore guided bio-isosteric replace
Autor:
Grant Wishart, Brian Montgomery, Anton Bom, Ronald Palin, Mark A. Weston, Andrea K. Houghton, Philip S. Jones, Helen Feilden, John K. Clark, Louise Evans
Publikováno v:
Bioorganicmedicinal chemistry. 15(4)
A series of 3-phenoxypropyl piperidine benzimidazol-2-one analogues have been discovered as novel NOP receptor agonists. Structure-activity relationships have been explored via N-3 substitution of the benzimidazol-2-one with a range of functionality.
Autor:
Ronald Palin, et al. et al.
Publikováno v:
ChemInform. 36