Previously reported propellane derivative KNT-42 preferred the κ receptor and functioned as a message part in the message-address concept, but its affinity for the κ receptor was not high. To improve affinity, we synthesized five pentacyclic propellane derivatives designed for the purpose of fixing the conformation of KNT-42. The etheno- and ethano-bridged derivatives SYK-347 and SYK-393 exhibited high affinity and selectivity for the κ receptor, whereas the other derivatives did not. These results would be due to the different ranges of movement of the basic nitrogens and less basicity of the nitrogens due to the electron withdrawing effect of the introduced hydroxy or keto group. SYK-347 and SYK-393 preferring the κ receptor were expected to be useful for designing selective ligands for opioid receptor types, especially the κ receptor.

译文

先前报道的推进烷衍生物KNT-42更喜欢 κ 受体,并在消息地址概念中充当消息部分,但其对 κ 受体的亲和力不高。为了提高亲和力,我们合成了五个五环推进烷衍生物,目的是固定KNT-42的构象。etheno和ethano桥接的衍生物SYK-347和SYK-393对 κ 受体表现出高亲和力和选择性,而其他衍生物则没有。这些结果是由于碱性氮的运动范围不同,而由于引入的羟基或酮基的吸电子效应,氮的碱度较低。优选 κ 受体的SYK-347和SYK-393被认为可用于设计阿片受体类型的选择性配体,尤其是 κ 受体。

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