Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10588329 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
Highly potent and selective small molecule neuropeptide Y Y2 receptor antagonists are reported. The systematic SAR exploration of a hit molecule N-(4-ethoxyphenyl)-4-[hydroxy(diphenyl)methyl]piperidine-1-carbothioamide, identified from HTS, led to the discovery of highly potent NPY Y2 antagonists 16 (CYM 9484) and 54 (CYM 9552) with IC50 values of 19Â nM and 12Â nM respectively.
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Authors
Gopi Kumar Mittapalli, Danielle Vellucci, Jun Yang, Marion Toussaint, Shaun P. Brothers, Claes Wahlestedt, Edward Roberts,