The identification and optimisation of novel and selective diamide neuropeptide Y Y2 receptor antagonists.

Lunniss, Gillian E; Barnes, Ashley A; Barton, Nick; Biagetti, Matteo; Bianchi, Federica; Blowers, Stephen M; Caberlotto, Laura; Emmons, Amanda; Holmes, Ian P; Montanari, Dino; Norris, Ros; Walters, Dewi J; Watson, Steve P

Lunniss, Gillian E; Barnes, Ashley A; Barton, Nick; Biagetti, Matteo; Bianchi, Federica; Blowers, Stephen M; Caberlotto, Laura; Emmons, Amanda; Holmes, Ian P; Montanari, Dino; Norris, Ros; Walters, Dewi J; Watson, Steve P.

Affiliation

Lunniss GE; GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Harlow, UK.

Bioorg Med Chem Lett ; 19(15): 4022-5, 2009 Aug 01.

Article in En | MEDLINE | ID: mdl-19581086

ABSTRACT

ABSTRACT

A novel small molecule NPY Y2 antagonist (3) identified from high throughput screening is described. 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.

Subject(s)

Amides/chemistry; Arginine/analogs & derivatives; Benzazepines/pharmacology; Receptors, Neuropeptide Y/antagonists & inhibitors; Receptors, Neuropeptide Y/chemistry; Animals; Arginine/pharmacology; Chemistry, Organic/methods; Chemistry, Pharmaceutical/methods; Drug Design; Humans; Inhibitory Concentration 50; Models, Chemical; Peptide Fragments/chemistry; Protein Binding; Rats; Structure-Activity Relationship

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Arginine / Benzazepines / Receptors, Neuropeptide Y / Amides Type of study: Diagnostic_studies Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2009 Type: Article Affiliation country: United kingdom

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