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The identification and optimisation of novel and selective diamide neuropeptide Y Y2 receptor antagonists |
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| Authors: | Gillian E. Lunniss Ashley A. Barnes Nick Barton Matteo Biagetti Federica Bianchi Stephen M. Blowers Laura Caberlotto Amanda Emmons Ian P. Holmes Dino Montanari Ros Norris Dewi J. Walters Steve P. Watson |
| Affiliation: | 1. GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Harlow, UK;2. Molecular Discovery Research, New Frontiers Science Park, Harlow, UK;3. Neurosciences Centre of Excellence for Drug Discovery, Medicine Research Centre, Verona, Italy |
| 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. |
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