刚性双环[3.1.0]己烷支架限制组胺的构象，提供选择性 H 受体配体。
Conformational Restriction of Histamine with a Rigid Bicyclo[3.1.0]hexane Scaffold Provided Selective H Receptor Ligands.
机构信息
Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan.
Center for Pharma-Food Research (CPFR), Graduate School of Pharmaceutical Sciences, University of Shizuoka, 52-1, Yada, Suruga-ku, Shizuoka 422-8526, Japan.
出版信息
Molecules. 2020 Aug 5;25(16):3562. doi: 10.3390/molecules25163562.
We designed and synthesized conformationally rigid histamine analogues with a bicyclo[3.1.0]hexane scaffold. All the compounds were selectively bound to the H receptor subtype over the H receptor subtype. Notably, compound showed potent binding affinity and over 100-fold selectivity for the H receptors ( = 5.6 nM for H and 602 nM for H). These results suggest that the conformationally rigid bicyclo[3.1.0]hexane structure can be a useful scaffold for developing potent ligands selective for the target biomolecules.
我们设计并合成了具有双环[3.1.0]己烷骨架的刚性组氨酸类似物。所有化合物均选择性地与 H 受体亚型结合，而不是 H 受体亚型。值得注意的是，化合物对 H 受体具有很强的结合亲和力和超过 100 倍的选择性（H 受体的 = 5.6 nM，H 受体的 = 602 nM）。这些结果表明，构象刚性的双环[3.1.0]己烷结构可以作为开发针对靶标生物分子的有效配体的有用支架。
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