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

GK Mittapalli, D Vellucci, J Yang, M Toussaint…

文献索引：Mittapalli, Gopi Kumar; Vellucci, Danielle; Yang, Jun; Toussaint, Marion; Brothers, Shaun P.; Wahlestedt, Claes; Roberts, Edward Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 12 p. 3916 - 3920

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被引用次数: 11

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.