作为强效和选择性M2毒蕈碱受体拮抗剂的醚类似物的设计与合成。
Design and synthesis of ether analogues as potent and selective M2 muscarinic receptor antagonists.
作者信息
Wang Y, Chackalamannil S, Chang W, Greenlee W, Ruperto V, Duffy R A, McQuade R, Lachowicz J E
机构信息
Schering-Plough Research Institute, Kenilworth, NJ 07033, USA.
出版信息
Bioorg Med Chem Lett. 2001 Apr 9;11(7):891-4. doi: 10.1016/s0960-894x(01)00100-7.
Abstract
Novel, selective M2 muscarinic antagonists, which replace the metabolically labile styrenyl moiety of the prototypical M2 antagonist 1 with an ether linkage, were synthesized. A detailed SAR study in this class of compounds has yielded highly active compounds that showed M2 Ki values of < 1.0 nM and >100-fold selectivity against M1, M3, and M5 receptors.
摘要
合成了新型的选择性M2毒蕈碱拮抗剂，其用醚键取代了原型M2拮抗剂1中代谢不稳定的苯乙烯基部分。对这类化合物进行的详细构效关系研究产生了高活性化合物，这些化合物的M2 Ki值<1.0 nM，对M1、M3和M5受体的选择性大于100倍。
Zotero 插件