奥贝林生长抑素sst1受体拮抗剂的芳基哌嗪部分的比吸收率
SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists.
作者信息
Hurth Konstanze, Enz Albert, Floersheim Philipp, Gentsch Conrad, Hoyer Daniel, Langenegger Daniel, Neumann Peter, Pfäffli Paul, Sorg Dieter, Swoboda Robert, Vassout Annick, Troxler Thomas
机构信息
Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
出版信息
Bioorg Med Chem Lett. 2007 Jul 15;17(14):3988-91. doi: 10.1016/j.bmcl.2007.04.078. Epub 2007 Apr 30.
The SAR of over 50 derivatives of octahydrobenzo[g]quinoline (obeline)-type somatostatin sst(1) receptor antagonist 1 is presented, focusing on the modification of its arylpiperazine moiety. Sst(1) affinities in this series cover a range of five orders of magnitude with the best derivatives displaying subnanomolar sst(1) affinities and >10,000-fold selectivities over the sst(2) receptor subtype as well as promising pharmacokinetic properties.
本文介绍了八氢苯并[g]喹啉（奥贝林）型生长抑素sst(1)受体拮抗剂1的50多种衍生物的构效关系，重点关注其芳基哌嗪部分的修饰。该系列中sst(1)亲和力涵盖五个数量级，最佳衍生物显示出亚纳摩尔级的sst(1)亲和力，对sst(2)受体亚型具有>10000倍的选择性以及良好的药代动力学性质。
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