1-Phenyl-8-azabicyclo[3.2.1]octane ethers:: A novel series of neurokinin (NK1) antagonists
1-Phenyl-8-azabicyclo[3.2.1]octane ethers:: A novel series of neurokinin (NK1) antagonists
复制标题
DOI：
10.1016/j.bmcl.2005.12.069
复制
发表时间：
2006-04-01
影响因子：
2.7
通讯作者：
Kulagowski, JJ
中科院分区：
文献类型：
--
作者：
Huscroft, IT;Carlson, EJ;Kulagowski, JJ
1-苯基-8-氮杂双环[3.2.1]辛烷醚是NK 1受体拮抗剂。在6-exo-位置的取代导致高亲和力的NK 1拮抗剂在体内具有延长的作用持续时间。在侧苯甲基醚侧链中引入α-甲基取代基得到对hERG通道具有增加的选择性的化合物。(C)2006爱思唯尔有限公司保留所有权利。
1-Phenyl-8-azabicyclo[3.2.1]octane ethers are NK1 receptor antagonists. Substitution at the 6-exo-position led to high affinity NK1 antagonists with a prolonged duration of action in vivo. Incorporation of an alpha-methyl substituent in the pendent benzyl ether side chain gave compounds with increased selectivity over the hERG channel. (C) 2006 Elsevier Ltd. All rights reserved.