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Your search keyword '"Elena Mezzogori"' showing total 3 results
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3 results on '"Elena Mezzogori"'

1. N′,2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II

Author

Jason M, Elliott, Robert W, Carling, Gary G, Chicchi, James, Crawforth, Peter H, Hutson, A Brian, Jones, Sarah, Kelly, Rose, Marwood, Georgina, Meneses-Lorente, Elena, Mezzogori, Fraser, Murray, Michael, Rigby, Inmaculada, Royo, Michael G N, Russell, Duncan, Shaw, Bindi, Sohal, Kwei Lan, Tsao, and Brian, Williams more...

Subjects
Neurotransmitter Agents, Dose-Response Relationship, Drug, Organic Chemistry, Clinical Biochemistry, Administration, Oral, Pharmaceutical Science, Receptors, Neurokinin-3, CHO Cells, Fluorine, Biochemistry, Piperazines, Structure-Activity Relationship, Hydrazines, Cricetinae, Drug Discovery, Quinolines, Tumor Cells, Cultured, Animals, Molecular Medicine, Molecular Biology
Abstract

Introduction of selected amine containing side chains into the 3-position of N',2-diphenylquinoline-4-carbohydrazide based NK3 antagonists abolishes unwanted hPXR activation. Introduction of a fluorine at the 8-position is necessary to minimize unwanted hI(Kr) affinity and a piperazine N-tert-butyl group is necessary for metabolic stability. The lead compound (8m) occupies receptors within the CNS following oral dosing (Occ(90) 7 mg/kg po; plasma Occ(90) 0.4 microM) and has good selectivity and excellent PK properties. more...

Published
2006
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2. N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists

Author

Gary G. Chicchi, Mark Stuart Chambers, Michael G. N. Russell, A. Brian Jones, Bindi Sohal, Robert W. Carling, Kwei lan Tsao, Georgina Meneses-Lorente, Inmaculada Royo, Peter H. Hutson, Jason Matthew Elliott, Michael Rigby, Brian John Williams, Elena Mezzogori, Rose Marwood, Fraser Murray, and Angus Murray Macleod more...

Subjects
Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Administration, Oral, CHO Cells, Carbohydrazide, Gerbil, Biochemistry, Chemical synthesis, chemistry.chemical_compound, Structure-Activity Relationship, Cricetinae, Drug Discovery, Tumor Cells, Cultured, Structure–activity relationship, Animals, Receptor, Molecular Biology, Neurotransmitter Agents, Dose-Response Relationship, Drug, Organic Chemistry, Antagonist, Receptors, Neurokinin-3, Hydrazines, chemistry, Quinolines, Molecular Medicine, Lead compound, Ex vivo
Abstract

A new class of potent NK3R antagonists based on the N',2-diphenylquinoline-4-carbohydrazide core is described. In an ex vivo assay in gerbil, the lead compound 2g occupies receptors within the CNS following oral dosing (Occ(90) 30 mg/kg po; plasma Occ(90) 0.95 microM) and has good selectivity and promising PK properties. more...

Published
2006

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3. Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety

Author

Robert W. Carling, Elena Mezzogori, Spencer J. Tye, Rebecca Dias, Rachael Lincoln, Alison J. Smith, María Domínguez, Keith A. Wafford, Frances A. Bromidge, Simon Charles Goodacre, Susan M. Cook, Robert J. Newman, Andrew Pike, David James Hallett, Atack, Michael G. N. Russell, Wayne F. A. Sheppard, Pushpinder Ferris, Michael Reader, Leslie J. Street, George R. Marshall, Bindi Sohal, Joanna Stanley, Castro Jl, and David S. Reynolds more...

Subjects
Agonist, Patch-Clamp Techniques, medicine.drug_class, Stereochemistry, Biphenyl derivatives, Biological Availability, Chemical synthesis, Receptor subtype, Radioligand Assay, Structure-Activity Relationship, Drug Discovery, medicine, Functional selectivity, Animals, Humans, GABA-A Receptor Agonists, Saimiri, GABAA receptor, Chemistry, Triazines, Imidazoles, Subtype selective, Receptors, GABA-A, Rats, Anti-Anxiety Agents, Molecular Medicine, Anxiety, medicine.symptom, Half-Life
Abstract

The identification of a series of imidazo[1,2-b][1,2,4]triazines with high affinity and functional selectivity for the GABA(A) alpha3-containing receptor subtype is described, leading to the identification of a clinical candidate, 11. Compound 11 shows good bioavailability and half-life in preclinical species, and it is a nonsedating anxiolytic in both rat and squirrel monkey behavioral models. more...

Published
2006