来源于（+）-3-蒈烯的吡唑衍生物；新型强效、选择性的鞘氨醇-1-磷酸（S1P（1））受体激动剂骨架。
Pyrazole derived from (+)-3-carene; a novel potent, selective scaffold for sphingosine-1-phosphate (S1P(1)) receptor agonists.
机构信息
Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
出版信息
Bioorg Med Chem Lett. 2010 Jan 1;20(1):35-7. doi: 10.1016/j.bmcl.2009.11.045. Epub 2009 Nov 15.
PMID:19954976
Abstract
High throughput screening and hit to lead optimization led to the identification of 'carene' as a promising scaffold showing selective S1P(1) receptor agonism. In parallel to this work we have established a pharmacophore model for the S1P(1) receptor highlighting the minimal structural requirement necessary for potent receptor agonism.
摘要
高通量筛选和命中到先导化合物优化导致了 'carene' 的鉴定，它是一种有前途的支架，显示出选择性 S1P(1)受体激动作用。在进行这项工作的同时，我们还建立了 S1P(1)受体的药效团模型，突出了强效受体激动作用所必需的最小结构要求。
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