Synthesis and Effects on the COX‐1 and COX‐2 Activity in Human Whole Blood ex vivo of Derivatives Containing the [1]Benzothienol‐[3, 2‐ d ]pyrimidin‐4‐one Heterocyclic System

Methyl and phenyl derivatives containing the [1]Benzothieno [3, 2‐ d ]pyrimidin‐4‐one system have been synthesized and tested as inhibitors of COX‐1 and COX‐2 activities in human whole blood (HWB) ex vivo ; all compounds turned out to be weak inhibitors of COX‐1 activity, as deduced from the TXB 2 (thromboxane B) generation; the acid phenyl derivative 11 b was an interesting inhibitor of COX‐2 activity, as deduced from the PGE 2 (prostaglandine E) generation.