Simplified YM-26734 inhibitors of secreted phospholipase A2 group IIA

Simplified analogs of YM-26734, a known inhibitor of secreted phospholipase A2 (sPLA2) group IIA, were synthesized and found to also display potent inhibition at low nanomolar concentrations. Analogs were based on the didodecanoylphloroglucinol portion of YM-26734 which contains the predicted active site calcium binding group.

Modeling of YM-26734 in the active site of secreted phospholipase A2 group IIA led to the design and synthesis of simplified analogs retaining nanomolar potency.Figure optionsDownload as PowerPoint slide