基于苯并咪唑酮的血清素5-HT1A或5-HT7R配体：合成与生物学评价。
Benzimidazolone-based serotonin 5-HT1A or 5-HT7R ligands: synthesis and biological evaluation.
作者信息
Badarau Eduard, Suzenet Franck, Bojarski Andrzej J, Fînaru Adriana-Luminiţa, Guillaumet Gérald
机构信息
Institut de Chimie Organique et Analytique, Université d'Orléans, UMR-CNRS 6005, UFR Sciences - BP 6759, rue de Chartres, 45067 Orléans Cedex 2, France.
出版信息
Bioorg Med Chem Lett. 2009 Mar 15;19(6):1600-3. doi: 10.1016/j.bmcl.2009.02.008. Epub 2009 Feb 8.
A new group of serotoninergic 5-HT(1A) or 5-HT(7) receptor ligands was identified. These compounds were designed and synthesized on a benzimidazolone scaffold and they enrich the well-known arylpiperazine class of 5-HT ligands. Diverse pharmacomodulations induced a shift in the affinity and selectivity profile with final identification of new potent hits.
已鉴定出一组新的血清素能5-HT(1A)或5-HT(7)受体配体。这些化合物是在苯并咪唑酮骨架上设计和合成的，它们丰富了著名的5-HT配体芳基哌嗪类。多种药效调节导致亲和力和选择性分布发生变化，最终鉴定出了新的有效活性化合物。
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