Synthesis and SAR of selective small molecule neuropeptide Y Y2 receptor antagonists.

Gopi Kumar Mittapalli,Danielle Vellucci,Jun Yang,Marion Toussaint,Shaun P Brothers,Claes Wahlestedt,Edward Roberts

Bioorganic & Medicinal Chemistry Letters（2012）

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摘要

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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关键词

Neuropeptide Y Y2,Antagonist,Structure–activity relationship,Thiourea,Carbamate

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