Research Topics
| Matteo BiagettiSummaryAffiliation: GlaxoSmithKline Research and Development Country: USA Publications
| Collaborators
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Detail Information
Publications
Synthesis and structure-activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiazol-2-amines derivatives as NPY Y5 antagonistsMatteo Biagetti
GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, Medicines Research Centre, Verona, Italy
Bioorg Med Chem Lett 20:4741-4. 2010..1.0]hexane scaffold was identified through modification of a screening hit. Structure-activity relationships and efforts undertaken to achieve a favourable pharmacokinetic profile in rat are described...
The identification of a series of novel, soluble non-peptidic neuropeptide Y Y2 receptor antagonistsGillian E Lunniss
GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Harlow, UK
Bioorg Med Chem Lett 20:7341-4. 2010..The identification and subsequent optimisation of a selective non-peptidic NPY Y2 antagonist series is described. This led to the development of amine 2, a selective, soluble NPY Y2 receptor antagonist with enhanced CNS exposure...
Design, synthesis and SAR of a novel series of benzimidazoles as potent NPY Y5 antagonistsDomenica Antonia Pizzi
GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, Medicines Research Centre, Verona, Italy
Bioorg Med Chem Lett 20:7120-3. 2010..Optimisation led to the identification of the brain penetrant, orally bioavailable Y5 antagonist 9b which significantly inhibited the food intake induced by a Y5 selective agonist with a minimal effective dose of 30mg/kg po...
Discovery and structure-activity relationship of a novel spirocarbamate series of NPY Y5 antagonistsColin P Leslie
Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline SpA, Medicines Research Centre, Verona, Italy
Bioorg Med Chem Lett 20:6103-7. 2010..Both compounds significantly inhibited the food intake induced by a Y5 selective agonist with minimal effective doses of 3mg/kg po...
The identification and optimisation of novel and selective diamide neuropeptide Y Y2 receptor antagonistsGillian E Lunniss
GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Harlow, UK
Bioorg Med Chem Lett 19:4022-5. 2009..A subsequent SAR study and optimisation programme based around this molecule is also described, leading to the identification of potent and soluble pyridyl analogue 36...
