特殊的麦角林类化合物是趋化因子受体 CXCR3 的高选择性、强效拮抗剂：有前途先导化合物的发现、特征描述和初步 SAR 研究。
Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: discovery, characterization and preliminary SAR of a promising lead.
机构信息
Novartis Institutes for BioMedical Research, Forum 1, Novartis Campus, CH-4056 Basel, Switzerland.
出版信息
Bioorg Med Chem Lett. 2009 Nov 1;19(21):6185-8. doi: 10.1016/j.bmcl.2009.09.002. Epub 2009 Sep 6.
PMID:19783143
Abstract
The special ergoline 1 is a highly potent, selective antagonist of the chemokine receptor CXCR3. The surprising selectivity of this LSD-related compound can be explained by different electronic and steric properties of the ergoline core structure caused by the urea portion of the molecule. Discovery, biopharmaceutical properties and first derivatives of this promising lead compound are discussed.
摘要
特殊麦角碱 1 是一种高活性、高选择性的趋化因子受体 CXCR3 拮抗剂。这种 LSD 相关化合物的惊人选择性可以通过分子的脲部分引起的麦角碱核心结构的不同电子和空间性质来解释。讨论了该有前途的先导化合物的发现、生物制药特性和第一个衍生物。
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