N'-氰基-4-(2-苯乙酰基)-N-邻甲苯基哌嗪-1-甲脒P2X7拮抗剂的合成及体外活性
Synthesis and in vitro activity of N'-cyano-4-(2-phenylacetyl)-N-o-tolylpiperazine-1-carboximidamide P2X7 antagonists.
作者信息
Morytko Michael J, Betschmann Patrick, Woller Kevin, Ericsson Anna, Chen Haipeng, Donnelly-Roberts Diana L, Namovic Marian T, Jarvis Michael F, Carroll William A, Rafferty Paul
机构信息
Abbott Bioresearch Center, Department of Medicinal Chemistry, 381 Plantation Street, Worcester, MA 01605, USA.
出版信息
Bioorg Med Chem Lett. 2008 Mar 15;18(6):2093-6. doi: 10.1016/j.bmcl.2008.01.094. Epub 2008 Jan 30.
A novel series of cyanoguanidine-piperazine P2X(7) antagonists was designed based upon the structure of A-740003. Structure-activity relationship (SAR) studies focused on the piperazine moiety and the right hand side substitution. Compounds were assayed for activity at human and rat P2X(7) receptors and compound 29 was found to possess potent activity (IC(50)=30-60 nM) at both species.
基于A-740003的结构设计了一系列新型的氰基胍-哌嗪P2X(7)拮抗剂。构效关系（SAR）研究聚焦于哌嗪部分和右侧取代基。对化合物进行了人源和大鼠P2X(7)受体活性测定，发现化合物29在这两个物种中均具有强效活性（IC(50)=30-60 nM）。
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