Exploratory study of oxatomide derivatives with high P2X7 receptor inhibitory activity
Exploratory study of oxatomide derivatives with high P2X7 receptor inhibitory activity
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具有高P2X7受体抑制活性的奥沙米特衍生物的探索性研究
DOI：
10.1016/j.bmcl.2022.129035
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发表时间：
2022
期刊：
影响因子：
--
通讯作者：
Matsuoka Isao
中科院分区：
文献类型：
--
作者：
Yamagiwa Noriyuki;Komine Mika;Hanaoka Fumi;Nobuta Tomoya;Yoshida Kazuki;Ito Masaaki;Matsuoka Isao
为了开发新型的P2X7R受体拮抗剂，人们设计并合成了多种草甘胺类化合物。对体内-体外P2X7R拮抗剂试验的评价表明，需要草原胺的DPM-哌嗪部分才能保持抑制活性。烷基链和芳香族头基的结构对P2X7R的抑制活性影响很大，C4型饱和烷基链和非取代或氟取代吲哚的类似物对P2X7R的拮抗作用是奥托米特的7.3~6.4倍。
Various oxatomide derivatives were designed and synthesized to develop novel P2X7receptor (P2X7R) antagonists. Evaluation forin-vitroP2X7R antagonist assay showed that DPM-piperazine moiety of oxatomide was required to maintain an inhibitory activity. The structure of both alkyl chains and aromatic head groups strongly affected P2X7R inhibitory activity, and the analogue, with C4-type saturated alkyl chain and a non-substituted or fluorine-substituted indole, was 7.3 to 6.4 times more potent as a P2X7R antagonist than oxatomide.