Exploratory study of oxatomide derivatives with high P2X7 receptor inhibitory activity,Bioorganic & Medicinal Chemistry Letters

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Exploratory study of oxatomide derivatives with high P2X7 receptor inhibitory activity
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2022-10-22 , DOI: 10.1016/j.bmcl.2022.129035
Noriyuki Yamagiwa ₁ , Mika Komine ₁ , Fumi Hanaoka ₁ , Tomoya Nobuta ₁ , Kazuki Yoshida ₁ , Masaaki Ito ₁ , Isao Matsuoka ₁

Affiliation

Various oxatomide derivatives were designed and synthesized to develop novel P2X₇ receptor (P2X₇R) antagonists. Evaluation for in-vitro P2X₇R 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.

中文翻译：

具有高P2X7受体抑制活性的oxatomide衍生物的探索性研究

设计并合成了各种草胺衍生物以开发新型 P2X ₇受体 (P2X ₇ R) 拮抗剂。体外P2X ₇ R 拮抗剂测定的评估表明，需要 Oxatomide 的 DPM-哌嗪部分来维持抑制活性。烷基链和芳族头基的结构强烈影响 P2X ₇ R 抑制活性，具有 C4 型饱和烷基链和未取代或氟取代吲哚的类似物的效力是 P2X 的 7.3 至 6.4 倍₇ R拮抗剂优于oxatomide。

更新日期：2022-10-22

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