Synthesis and SAR of selective small molecule neuropeptide Y Y2 receptor antagonists |
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| Authors: | Mittapalli Gopi Kumar Vellucci Danielle Yang Jun Toussaint Marion Brothers Shaun P Wahlestedt Claes Roberts Edward |
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| Institution: | Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Rd, La Jolla, CA 92037, USA. |
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| 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 IC(50) values of 19 nM and 12 nM respectively. |
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