Search Results - "Morphy, J. Richard"
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Identification and optimisation of novel sulfonamide, selective vasopressin V₁B receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-06-2011)“…The synthesis and preliminary structure–activity relationships (SAR) of a novel class of vasopressin V₁B receptor antagonists are described. Hit compound 5,…”
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2
Synthesis and SAR studies of novel 2-(6-aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide Vasopressin V₁b receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-06-2011)“…Synthesis and structure–activity relationships (SAR) of a novel series of vasopressin V₁b antagonists are described…”
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3
Reagent concentration effects in the REM resin solid phase synthesis of tertiary amines
Published in Tetrahedron (17-03-2003)“…The use of reagent concentration has resulted in increased rates for all stages of the REM resin synthesis of tertiary amines. These increases in rate…”
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4
Synthesis and SAR studies of novel 2-(6-aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4 H)-yl)acetamide Vasopressin V 1b receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-06-2011)“…Synthesis and structure–activity relationships (SAR) of a novel series of vasopressin V 1b antagonists are described…”
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5
Identification and optimisation of novel sulfonamide, selective vasopressin V 1B receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-06-2011)“…The synthesis and preliminary structure–activity relationships (SAR) of a novel class of vasopressin V 1B receptor antagonists are described. Hit compound 5,…”
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6
Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist
Published in Bioorganic & medicinal chemistry letters (01-01-2011)“…High-throughput screening of 3.87million compounds delivered a novel series of non-steroidal GR antagonists. Subsequent rounds of optimisation allowed…”
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7
Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V₁b receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-03-2011)“…Synthesis and structure–activity relationships (SAR) of a novel series of vasopressin V₁b (V₃) antagonists are described…”
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8
Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4 H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-09-2010)“…The discovery, synthesis, and preliminary structure–activity relationship (SAR) of a novel class of vasopressin V3 (V1b) receptor antagonists is described…”
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9
Synthesis of Tertiary Amines Using a Polystyrene (REM) Resin
Published in Journal of the American Chemical Society (09-04-1997)“…A range of tertiary amines was constructed using a “traceless” linker on a polystyrene resin (REM resin), starting from secondary amines, primary amines, and…”
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10
The First Potent and Selective Inhibitors of the Glycine Transporter Type 2
Published in Journal of medicinal chemistry (16-08-2001)Get full text
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11
Synthesis of an array of amides by aluminium chloride assisted cleavage of resin-bound esters
Published in Tetrahedron letters (29-04-1996)“…A new method for the synthesis of amino amides using Wang or Tentagel-PHB resins is described. The method uses aluminium chloride to promote the conversion of…”
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12
2-(Aminomethyl)-benzamide-based glycine transporter type-2 inhibitors
Published in Bioorganic & medicinal chemistry letters (19-01-2004)“…Structure–activity studies on benzamide 1 obtained from library screening led to the discovery of a novel series of potent and selective glycine transporter…”
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13
Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists
Published in Bioorganic & medicinal chemistry letters (01-02-2005)“…A series of potent and soluble ORL1 agonists was prepared and evaluated. Compound 41 showed antinociceptive properties in mouse formalin paw test (ED 50 = 1.07…”
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14
Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4 H)-yl)acetamide vasopressin V 1b receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-03-2011)“…Synthesis and structure–activity relationships (SAR) of a novel series of vasopressin V 1b (V 3) antagonists are described. 2-(4-Oxo-2-aryl-quinazolin-3(4…”
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15
Optimization of Reaction Conditions for REM Resin-Bound Quaternization Reactions
Published in Journal of combinatorial chemistry (01-05-2002)“…A study into the effect of reaction variables on the quaternization of REM resin-bound tertiary amines was undertaken. The influence of resin matrix, solvent,…”
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16
A novel linker strategy for solid-phase synthesis
Published in Tetrahedron letters (29-04-1996)“…The REM resin for solid phase synthesis is described. Its use is illustrated by preparing a small array of tertiary amines using a Hofmann elimination…”
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17
Solid-Phase Synthesis of Cyclic Imides
Published in Journal of combinatorial chemistry (01-03-1999)“…A cyclative cleavage strategy for the synthesis of cyclic imides on a polystyrene resin is described. After optimization of the cleavage conditions, a small…”
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18
Low dilution procedures in solid-phase organic synthesis: Diels–Alder and Heck reactions
Published in Tetrahedron letters (19-08-2002)“…The use of extremely low solvent volumes (2 μL or less per mg resin) results in significant increases in yield for both the Diels–Alder and Heck reactions on…”
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19
Fluorocarbon accelerated supported transformations (FAST) on REM resin
Published in Tetrahedron letters (15-10-2001)“…The use of perfluorous organic solvents in the solid-phase synthesis of 3° amines on REM resin allows a large reduction in both reaction time and the amount of…”
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Design and Synthesis of a Maximally Diverse and Druglike Screening Library Using REM Resin Methodology
Published in Journal of combinatorial chemistry (01-11-2001)“…A 3042 compound screening library was synthesized using a combination of two solid-phase technologies: REM resin methodology and Lewis acid promoted…”
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