Search Results - "Merchant, Kevin J."

8-Fluoroimidazo[1,2-a]pyridine: Synthesis, physicochemical properties and evaluation as a bioisosteric replacement for imidazo[1,2-a]pyrimidine in an allosteric modulator ligand of the GABAA receptor by Humphries, Alexander C., Gancia, Emanuela, Gilligan, Myra T., Goodacre, Simon, Hallett, David, Merchant, Kevin J., Thomas, Steve R.

“…8-Fluoroimidazo[1,2-a]pyridine has been established as a physicochemical mimic of imidazo[1,2-a]pyrimidine, using both in silico and traditional techniques…”
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Selective, Orally Active γ-Aminobutyric AcidA α5 Receptor Inverse Agonists as Cognition Enhancers by Sternfeld, Francine, Carling, Robert W, Jelley, Richard A, Ladduwahetty, Tamara, Merchant, Kevin J, Moore, Kevin W, Reeve, Austin J, Street, Leslie J, O'Connor, Desmond, Sohal, Bindi, Atack, John R, Cook, Susan, Seabrook, Guy, Wafford, Keith, Tattersall, F. David, Collinson, Neil, Dawson, Gerard R, Castro, José L, MacLeod, Angus M

“…Nonselective inverse agonists at the γ-aminobutyric acidA (GABA-A) benzodiazepine binding site have cognition-enhancing effects in animals but are anxiogenic…”
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Non-basic ligands for aminergic GPCRs: The discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders by Ladduwahetty, Tammy, Gilligan, Myra, Humphries, Alexander, Merchant, Kevin J., Fish, Rebecca, McAlister, George, Ivarsson, Magnus, Dominguez, Maria, O’Connor, Desmond, MacLeod, Angus M.

“…Herein is described the development of a non-basic series of aryl sulfones as 5-HT2A receptor antagonists with excellent receptor occupancy on oral dosing in…”
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Tryptophan-Derived NK1 Antagonists: Conformationally Constrained Heterocyclic Bioisosteres of the Ester Linkage by Lewis, Richard T, Macleod, Angus M, Merchant, Kevin J, Kelleher, Fintan, Sanderson, Ian, Herbert, Richard H, Cascieri, Margaret A, Sadowski, Sharon, Ball, Richard G, Hoogsteen, Karst

“…The 3,5-bis(trifluoromethyl)benzyl ester of N-acetyl-L-tryptophan 1 (L-732,138) has been identified previously as a potent and selective substance P receptor…”
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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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Potassium trimethylsilanolate mediated hydrolysis of nitriles to primary amides by Merchant, Kevin J

“…Treatment of nitriles with potassium trimethylsilanolate under mild anhydrous conditions readily yields the corresponding primary amides after a simple aqueous…”
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4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia by Fish, L Rebecca, Gilligan, Myra T, Humphries, Alexander C, Ivarsson, Magnus, Ladduwahetty, Tammy, Merchant, Kevin J, O'Connor, Desmond, Patel, Smita, Philipps, Elisabeth, Vargas, Hugo M, Hutson, Peter H, MacLeod, Angus M

“…Incorporation of fluorine at the 4-position of an existing series of sulfonyl piperidine 5-HT2A antagonists gave compounds with increased selectivity over the…”
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Novel quinuclidine-based ligands for the muscarinic cholinergic receptor by Saunders, John, Cassidy, Mark, Freedman, Stephen B, Harley, Elizabeth A, Iversen, Leslie L, Kneen, Clare, MacLeod, Angus M, Merchant, Kevin J, Snow, Roger J, Baker, Raymond

“…Recent clinical studies on Alzheimer's patients have implied that only agents displaying high efficacy at the cortical muscarinic receptor have yielded…”
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N-Acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists by MacLeod, Angus M, Merchant, Kevin J, Cascieri, Margaret A, Sadowski, Sharon, Ber, Elzbieta, Swain, Christopher J, Baker, Raymond

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4,4-Disubstituted Piperidine High-Affinity NK1 Antagonists:  Structure−Activity Relationships and in Vivo Activity by Stevenson, Graeme I, Huscroft, Ian, MacLeod, Angus M, Swain, Christopher J, Cascieri, Margaret A, Chicchi, Gary G, Graham, Michael I, Harrison, Timothy, Kelleher, Fintan J, Kurtz, Marc, Ladduwahetty, Tamara, Merchant, Kevin J, Metzger, Joseph M, MacIntyre, D. E, Sadowski, Sharon, Sohal, Balbinder, Owens, Andrew P

“…Previously reported studies from these laboratories described the design of a novel series of high-affinity NK1 antagonists based on the 4,4-disubstituted…”
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Identification of L-Tryptophan Derivatives with Potent and Selective Antagonist Activity at the NK1 Receptor by MacLeod, Angus M, Merchant, Kevin J, Brookfield, Frederick, Kelleher, Fintan, Stevenson, Graeme, Owens, Andrew P, Swain, Christopher J, Cascieri, Margaret A, Sadowski, Sharon

“…As part of a program of screening the Merck sample collection, N-ethyl-L-tryptophan benzyl ester was identified as a weak antagonist at the substance P (NK1)…”
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An Efficient Protocol for the Preparation of Primary Alcohols Bearing a β-Chiral Center via an Oxazolidinone Auxiliary Mediated Resolution, and Application to the Synthesis of 4,4-Disubstituted Piperidine Substance P Antagonists by Lewis, Richard T, Ladduwahetty, Tamara, Merchant, Kevin J, Keown, Linda E, Hitzel, Laure, Verrier, Hugh, Stevenson, Graeme I, MacLeod, Angus M

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Identification of a Series of 3-(Benzyloxy)-1-azabicyclo[2.2.2]octane Human NK1 Antagonists by Swain, Christopher J, Sewart, Eileen M, Cascieri, Margaret A, Fong, Tung M, Herbert, Richard, MacIntyre, D Euan, Merchant, Kevin J, Owen, Simon N, Owens, Andrew P

“…The synthesis and in vitro and in vivo evaluation of a series of 3-(benzyloxy)-1-azabicyclo-[2.2.2]octane NK1 antagonists are described. While a number of…”
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Synthesis and Biological Evaluation of NK1 Antagonists Derived from L-Tryptophan by MacLeod, Angus M, Cascieri, Margaret A, Merchant, Kevin J, Sadowski, Sharon, Hardwicke, Sarah, Lewis, Richard T, MacIntyre, D. Euan, Metzger, Joseph M, Fong, Tung Ming

“…The 3,5-bis(trifluoromethyl)benzyl ester of N-acetyl-L-tryptophan (3), which was derived from the screening lead N-ethyl-L-tryptophan benzyl ester, has been…”
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8-Fluoroimidazo[1,2-a]pyridine: synthesis, physicochemical properties and evaluation as a bioisosteric replacement for imidazo[1,2-a]pyrimidine in an allosteric modulator ligand of the GABA A receptor by Humphries, Alexander C, Gancia, Emanuela, Gilligan, Myra T, Goodacre, Simon, Hallett, David, Merchant, Kevin J, Thomas, Steve R

“…8-Fluoroimidazo[1,2-a]pyridine has been established as a physicochemical mimic of imidazo[1,2-a]pyrimidine, using both in silico and traditional techniques…”
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Synthesis and muscarinic activities of 1,2,4-thiadiazoles by MacLeod, Angus M, Baker, Raymond, Freedman, Stephen B, Patel, Shailendra, Merchant, Kevin J, Roe, Michael, Saunders, John

“…A series of novel 1,2,4-thiadiazoles bearing a mono- or bicyclic amine at C5 were prepared. Quinuclidine and 1-azabicyclo[2.2.1]heptane derivatives were…”
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8-Fluoroimidazo[1,2-a]pyridine: Synthesis, physicochemical properties and evaluation as a bioisosteric replacement for imidazo[1,2-a]pyrimidine in an allosteric modulator ligand of the GABA sub(A) receptor by Humphries, Alexander C, Gancia, Emanuela, Gilligan, Myra T, Goodacre, Simon, Hallett, David, Merchant, Kevin J, Thomas, Steve R

“…8-Fluoroimidazo[1,2-a]pyridine has been established as a physicochemical mimic of imidazo[1,2-a]pyrimidine, using both in silico and traditional techniques…”
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4-Fluorosulfonylpiperidines : Selective 5-HT2A ligands for the treatment of insomnia: G-protein-coupled receptors in drug discovery by FISH, L. Rebecca, GILLIGAN, Myra T, HUTSON, Peter H, MACLEOD, Angus M, HUMPHRIES, Alexander C, IVARSSON, Magnus, LADDUWAHETTY, Tammy, MERCHANT, Kevin J, O'CONNOR, Desmond, PATEL, Smita, PHILIPPS, Elisabeth, VARGAS, Hugo M

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4-Fluorosulfonylpiperidines: Selective 5-HT 2A ligands for the treatment of insomnia by Fish, L. Rebecca, Gilligan, Myra T., Humphries, Alexander C., Ivarsson, Magnus, Ladduwahetty, Tammy, Merchant, Kevin J., O’Connor, Desmond, Patel, Smita, Philipps, Elisabeth, Vargas, Hugo M., Hutson, Peter H., MacLeod, Angus M.

“…α-Fluorosulfones, of general structure 3, were synthesized as an alternative approach to reduce the p K a of the piperidine ring in an existing series of…”
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Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers by Sternfeld, Francine, Carling, Robert W, Jelley, Richard A, Ladduwahetty, Tamara, Merchant, Kevin J, Moore, Kevin W, Reeve, Austin J, Street, Leslie J, O'Connor, Desmond, Sohal, Bindi, Atack, John R, Cook, Susan, Seabrook, Guy, Wafford, Keith, Tattersall, F David, Collinson, Neil, Dawson, Gerard R, Castro, José L, MacLeod, Angus M

“…Nonselective inverse agonists at the gamma-aminobutyric acid(A) (GABA-A) benzodiazepine binding site have cognition-enhancing effects in animals but are…”
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