Search Results - "Showell, G A"

Silicon switches of marketed drugs by Pooni, P K, Showell, G A

“…The application of organosilicon chemistry is a strategy to develop best in class drugs applied to targets that have been validated as tractable and drug-able…”
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Chemistry challenges in lead optimization: silicon isosteres in drug discovery by Showell, Graham A, Mills, John S

“…During the lead optimization phase of drug discovery projects, the factors contributing to subsequent failure might include poor portfolio decision-making and…”
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Synthesis and biological activity of 1,2,4-oxadiazole derivatives: highly potent and efficacious agonists for cortical muscarinic receptors by Street, Leslie J, Baker, Raymond, Book, Tracey, Kneen, Clare O, MacLeod, Angus M, Merchant, Kevin J, Showell, Graham A, Saunders, John, Herbert, Richard H

“…The synthesis and biochemical evaluation of novel 1,2,4-oxadiazole-based muscarinic agonists which can readily penetrate into the CNS is reported. Efficacy and…”
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Tetrahydropyridyloxadiazoles : semirigid muscarinic ligands by SHOWELL, G. A, GIBBONS, T. L, KNEEN, C. O, MACLEOD, A. M, MERCHANT, K, SAUNDERS, J, FREEDMAN, S. B, PATEL, S, BAKER, R

“…Recent studies have described novel azabicycle-based muscarinic agonists which readily penetrate into the central nervous system and are capable of displaying…”
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4-Hydroxy-1-[3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl]piperidines : Selective h5-HT1D agonists for the treatment of migraine by BOURRAIN, S, NEDUVELIL, J. G, BEER, M. S, STANTON, J. A, SHOWELL, G. A, MACLEOD, A. M

“…A series of 4-hydroxy-1-[3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl] piperidines was investigated as potential selective h5-HT1D agonists for the treatment…”
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Sila-venlafaxine, a Sila-Analogue of the Serotonin/Noradrenaline Reuptake Inhibitor Venlafaxine:  Synthesis, Crystal Structure Analysis, and Pharmacological Characterization by Daiss, Jürgen O, Burschka, Christian, Mills, John S, Montana, John G, Showell, Graham A, Warneck, Julie B. H, Tacke, Reinhold

“…The serotonin/noradrenaline reuptake inhibitor rac-1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexan-1-ol (rac-venlafaxine, rac-1a) is in clinical use…”
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L-687,306: a functionally selective and potent muscarinic M1 receptor agonist by Freedman, S B, Patel, S, Harley, E A, Iversen, L L, Baker, R, Showell, G A, Saunders, J, McKnight, A, Newberry, N, Scholey, K

“…The oxadiazole L-687,306 is a high affinity muscarinic agonist with a N-methylscopolamine/oxotremorine-M binding profile predictive of a partial agonist…”
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Selective thyromimetics. Cardiac-sparing thyroid hormone analogs containing 3'-arylmethyl substituents by Leeson, Paul D, Emmett, John C, Shah, Virendra P, Showell, Graham A, Novelli, Ricardo, Prain, H. Douglas, Benson, Martin G, Ellis, David, Pearce, Nigel J, Underwood, Anthony H

“…Introduction of specific arylmethyl groups at the 3'-position of the thyroid hormone 3,3',5-triiodo-L-thyronine (T3), and its known hormonally active…”
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Synthesis and antihypertensive activity of 6,7-disubstituted trans-4-amino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-3-ols by Evans, John M, Fake, Charles S, Hamilton, Thomas C, Poyser, Robert H, Showell, Graham A

“…A series of novel 6,7-disubstituted trans-3,4-dihydro-2, 2-dimethyl-4-pyrrolidino-(or piperidino)-2H-1-benzopyran-3-ols was prepared and tested for…”
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2-Methyl-1,3-dioxaazaspiro[4.5]decanes as novel muscarinic cholinergic agonists by Saunders, John, Showell, Graham A, Snow, Roger J, Baker, Raymond, Harley, Elizabeth A, Freedman, Stephen B

“…Many nonquaternary ammonium muscarinic agonists have been developed over the last few years, but most of the existing compounds (e.g., arecoline, RS-86, AF-30)…”
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High-Affinity and Potent, Water-Soluble 5-Amino-1,4-benzodiazepine CCKB/Gastrin Receptor Antagonists Containing a Cationic Solubilizing Group by Showell, Graham A, Bourrain, Sylvie, Neduvelil, Joseph G, Fletcher, Stephen R, Baker, Raymond, Watt, Alan P, Fletcher, Alan E, Freedman, Stephen B, Kemp, John A

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Approaches to rational drug development in Alzheimer's disease by Iversen, L L, Iversen, S D, Freedman, S B, Dawson, G, Rupniak, N, Hargreaves, R J, Showell, G A, Street, L J, Baker, R

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Design strategies for building drug-like chemical libraries by Mitchell, T, Showell, G A

“…There has been increased pressure over the last few years to design and synthesize chemical libraries that are more 'drug-like' in character. This review…”
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Exploitation of silicon medicinal chemistry in drug discovery by Mills, John S, Showell, Graham A

“…There remains considerable pressure on the pharmaceutical industry to increase productivity and reduce the attrition of drug candidates. Genomics, parallel…”
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Thyroid hormone analogs. Synthesis of 3'-substituted 3,5-diiodo-L-thyronines and quantitative structure-activity studies of in vitro and in vivo thyromimetic activities in rat liver and heart by Leeson, Paul D, Ellis, David, Emmett, John C, Shah, Virendra P, Showell, Graham A, Underwood, Anthony H

“…Twenty-nine novel 3'-substituted derivatives of the thyroid hormone 3,3',5-triiodo-L-thyronine (T3) have been synthesized by using established methods and by a…”
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Synthesis, Crystal Structure Analysis, and Pharmacological Characterization of Disila-bexarotene, a Disila-Analogue of the RXR-Selective Retinoid Agonist Bexarotene by Daiss, Jürgen O, Burschka, Christian, Mills, John S, Montana, John G, Showell, Graham A, Fleming, Ian, Gaudon, Claudine, Ivanova, Diana, Gronemeyer, Hinrich, Tacke, Reinhold

“…Twofold sila-substitution (C/Si exchange) in the saturated ring of the tetrahydronaphthalene skeleton of the RXR-selective retinoid agonist bexarotene (1a)…”
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( R)-Sila-venlafaxine: A selective noradrenaline reuptake inhibitor for the treatment of emesis by Showell, Graham A., Barnes, Matthew J., Daiss, Jürgen O., Mills, John S., Montana, John G., Tacke, Reinhold, Warneck, Julie B.H.

“…The in vitro profile and in vivo anti-emetic activity of the selective noradrenaline reuptake inhibitor ( R )- 2 are reported. Sila-substitution of drugs (the…”
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Substituted pyrazoles as novel selective ligands for the human dopamine D4 receptor by Bourrain, S, Collins, I, Neduvelil, J G, Rowley, M, Leeson, P D, Patel, S, Emms, F, Marwood, R, Chapman, K L, Fletcher, A E, Showell, G A

“…Two novel series of 3-(heterocyclylmethyl)pyrazoles have been synthesised and evaluated as ligands for the human dopamine D4 receptor. Compounds in series I…”
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Binding of 2,4-disubstituted morpholines at human D4 dopamine receptors by Showell, G A, Emms, F, Marwood, R, O'Connor, D, Patel, S, Leeson, P D

“…The synthesis of a series of 2,4-disubstituted morpholines is described and their affinities at human dopamine receptors reported. The orally bioavailable…”
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The design of a new potent and selective ligand for the orphan bombesin receptor subtype 3 (BRS3) by Boyle, Robert G., Humphries, John, Mitchell, Tim, Showell, Graham A., Apaya, Robert, Iijima, Hiroaki, Shimada, Hiroshi, Arai, Tomonori, Ueno, Hiroaki, Usui, Yoshihiro, Sakaki, Toshiro, Wada, Etsuko, Wada, Keiji

“…Extensive SAR studies on the unselective BRS3 agonist, [H‐D‐Phe6,β‐Ala11,Phe13,Nle14]‐bombesin‐(6‐14)‐nonapeptide amide, have highlighted structural features…”
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