Exploratory study of oxatomide derivatives with high P2X receptor inhibitory activity.

Various oxatomide derivatives were designed and synthesized to develop novel P2X receptor (P2XR) antagonists. Evaluation for in-vitro P2XR 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 P2XR inhibitory activity, and the analogue, with C4-type saturated alkyl chain and a non-substituted or fluorine-substituted indole, was 7.