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Exploratory study of oxatomide derivatives with high P2X7 receptor inhibitory activity
Noriyuki Yamagiwa1, Mika Komine1, Fumi Hanaoka1
1Takasaki University of Health and Welfare, 60, Nakaorui, Takasaki-city, Gunma 370-0033, Japan.
Abstract:
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.
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