Higginbottom M, Hill D R, Horwell D C, Mostafai E, Suman-Chauhan N, Roberts E
Parke-Davis Neuroscience Research Centre, Addenbrookes Hospital Site, Cambridge, U.K.
Bioorg Med Chem. 1993 Sep;1(3):209-17. doi: 10.1016/s0968-0896(00)82123-9.
The synthesis and structure-activity relationships (SAR) for a series of conformationally restricted analogues of the selective cholecystokinin (CCK) antagonist CI-988 and some closely related analogues are described. A series of appropriately substituted cis- and trans-amino decalins are prepared that mimic the through bond distances between the functional groups in the parent compound CI-988 whilst restricting bond rotation. This strategy has led to conformationally more rigid derivatives that have increased CCK-B receptor binding affinity.
本文描述了一系列选择性胆囊收缩素（CCK）拮抗剂CI-988的构象受限类似物以及一些密切相关类似物的合成与构效关系（SAR）。制备了一系列适当取代的顺式和反式氨基十氢萘，它们模拟母体化合物CI-988中官能团之间的通过键距离，同时限制键的旋转。该策略已产生构象更刚性的衍生物，其CCK-B受体结合亲和力增加。
