5‐HT7 Receptor Antagonists with an Unprecedented Selectivity Profile,ChemMedChem

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5‐HT7 Receptor Antagonists with an Unprecedented Selectivity Profile
ChemMedChem ( IF 3.6 ) Pub Date : 2018-03-30 , DOI: 10.1002/cmdc.201800026
Ali Ates ₁ , Pierre Burssens ₁ , Olivier Lorthioir ₁ , Patrick Lo Brutto ₁ , Gwenael Dehon ₁ , Jean Keyaerts ₁ , Francis Coloretti ₁ , Bénédicte Lallemand ₁ , Valérie Verbois ₁ , Michel Gillard ₁ , Céline Vermeiren ₁

Affiliation

Selective leads: In this study, we generated a new series of serotonin 5‐HT₇ receptor antagonists. Their synthesis, structure–activity relationships, and selectivity profiles are reported. This series includes 5‐HT₇ antagonists with unprecedented high selectivity for the 5‐HT₇ receptor, setting the stage for lead optimization of drugs acting on a range of neurological targets.

中文翻译：

具有前所未有的选择性特征的5‐HT7受体拮抗剂

选择性线索：在这项研究中，我们产生了一系列新的5-羟色胺5-HT ₇受体拮抗剂。报告了它们的合成，结构-活性关系和选择性概况。该系列包括对5-HT ₇受体具有空前的高选择性的5-HT ₇拮抗剂，为作用于一系列神经学靶标的药物的前导优化奠定了基础。

更新日期：2018-03-30

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