Synthesis and structure–activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor

High-throughput screening identified compound 1 as a potent P2X7 receptor antagonist suitable for lead optimisation. Structure–activity relationships (SAR) of a series of (1H-pyrazol-4-yl)acetamides were investigated and compound 32 was identified as a potent P2X7 antagonist with enhanced potency and favourable physicochemical and pharmacokinetic properties.

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