Zobrazeno 1 - 10
of 75
pro vyhledávání: '"David I. C. Scopes"'
Publikováno v:
Journal of the Chemical Society, Perkin Transactions 1. :2569-2576
7,8-Dichloro-1,2,3,4,5,6-hexahydrobenzo[ f ]quinolin-3-one 10 (R = H) is obtained by reaction of 5,6-dichloro-3,4-dihydronaphthalen-2(1H)-one pyrrolidine enamine 9 with acrylamide and is N-alkylated to 7,8-dichloro-1,2,3,4,5,6-hexahydro-4-propylbenzo
Autor:
David I. C. Scopes, Celestine T. O'Shaughnessy, J.C. Barnes, John W. Clitherow, Gavin J. Kilpatrick, Paul Beswick, J.D. Brown
Publikováno v:
European Journal of Pharmacology. 311:305-310
We have examined the specific binding of the tritiated derivative of the potent histamine H 3 receptor antagonist, [3,4- 3 H 2 ]-cyclohexyl-{[4-(3 H -imidazol-4-yl)-piperidin-1-yl]iminomethyl}-amine ([ 3 H]GR168320), to homogenates of rat cerebral co
Autor:
David I. C. Scopes, J. W. Clitherow, P. Beswick, J. Clapham, D. J. Evans, J.C. Barnes, W. J. Irving, A. G. Hayes, J.D. Brown
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:833-838
Replacement of the isothiourea moiety of known histamine H 3 antagonists by certain 5-membered heteroaromatic systems can give compounds with an improved activity profile. One of these, 3-[(4-chlorophenyl)methyl]-5-[2-(1H-imidazol-4-yl)ethyl] 1,2,4-o
Publikováno v:
Synlett. 2004:2776-2778
A β-lactam template has been used to induce the stereochemistry in a simple route to imino sugars.
Autor:
Elizabeth A. Graham, M. P. Turpin, David I. C. Scopes, Izaak Den Daas, Lee A. Harrison, David R. Bull, A. G. Hayes, Gavin J. Kilpatrick, Michael J. Sheehan, C. Large, M. R. Johnson, P. John Murray, Graeme Michael Robertson, Carole M. Stubbs
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:219-222
A novel series of arylpiperazines has been synthesised which show high affinity for dopamine D 3 receptors. Several of these compounds exhibit ca . 100 fold selectivity for the dopamine D 3 receptor over D 1 , D 2 and D 4 receptors. In vivo studies s
Autor:
M. C. Carter, Eric W. Collington, Feniuk W, M. Skingle, J. W. Clitherow, C. C. Jordan, Connor He, I. B. Campbell, Guy A. Higgins, David I. C. Scopes
Publikováno v:
Journal of Medicinal Chemistry. 37:2253-2257
Publikováno v:
Journal of Medicinal Chemistry. 37:2138-2144
The synthesis of 5-(arylacetyl)-4-[(alkylamino)methyl]furo[3,2-c]pyri- dines (16-23, 26, 27) and their activities as κ-opioid receptor agonists are described. κ-Agonist potency was particularly sensitive to the na- ture of the basic moiety. In part
Autor:
David I. C. Scopes
Publikováno v:
Expert Opinion on Investigational Drugs. 3:369-377
This article provides an overview of the development of selective K-opioid receptor antagonists as potential analgesics and neuroprotective agents. An important milestone in defining the properties of a K-receptor agonist was the discovery of the N-(
Autor:
Eugene, O'Hare, David I C, Scopes, J Mark, Treherne, John, Monaghan, Philip M, Palmer, Hozefa, Amijee, Eun-Mee, Kim
Publikováno v:
Journal of Alzheimer's disease : JAD. 25(2)
Behavioral effects of a novel anti-inflammatory SEN1176 were investigated. This pyrrolo[3,2-e][1,2,4]triazolo[1,5-a]pyrimidine suppresses amyloid-β (Aβ)1-42-induced macrophage production of nitric oxide, TNF-α, IL-1β, and IL-6 in a dose-dependent
Autor:
G.M. Drew, A. Travers, B.C. Ross, T.A. Panchal, E. Palmer, Steve P. Watson, A. Hilditch, David Middlemiss, J.G. Montana, M.J. Robertson, A.A.E. Hunt, G.R.M. Manchee, G.C. Hirst, J.M.S. Paton, T. Hubbard, David I. C. Scopes, G. Stuart, M.D. Dowle
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:2043-2046
A series of GR117289 derived amino acid-amide angiotensin II antagonists is described. The possibility that the amino acid-amide element of these molecules mimics the C-terminus of Angiotensin II is discounted. One of these compounds, (2g), exhibits