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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Aminopyrazoles with high affinity for the human neuropeptide Y5 receptor.
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Aminopyrazoles with high affinity for the human neuropeptide Y5 receptor.

机译:对人神经肽Y5受体具有高亲和力的氨基吡唑。

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摘要

1,3-Disubstituted-5-aminopyrazoles were prepared based on a lead compound found through high-throughput screening of our corporate compound library in an assay measuring affinity for the human neuropeptide Y5 receptor. The target compounds were prepared by cyclization of alpha-cyanoketones with appropriate hydrazines, followed by reduction and coupling to various sulfonamido-carboxylic acids. Several of these arylpyrazoles (e.g., 19 and 45) displayed high affinity for the human NPY Y5 receptor (<20nM IC(50)s).
机译:1,3-二取代的5-氨基吡唑类化合物是通过在对人神经肽Y5受体的亲和力测定中通过对我们的公司化合物库进行高通量筛选而发现的先导化合物制备的。通过将α-氰基酮与适当的肼环合,然后还原并偶联至各种磺酰胺基羧酸,来制备目标化合物。这些芳基吡唑中的几种(例如19和45)显示出对人NPY Y5受体的高亲和力(<20nM IC(50)s)。

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