Synthesis and SAR of selective small molecule neuropeptide Y Y2 receptor antagonists
2012
Mittapalli, Gopi Kumar | Vellucci, Danielle | Yang, Jun | Toussaint, Marion | Brothers, Shaun P. | Wahlestedt, Claes | Roberts, Edward
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 19nM and 12nM respectively.
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