132131-85-2Relevant academic research and scientific papers
Design and synthesis of a series of glycerol-derived receptor mediated calcium entry (RMCE) blockers
Howson,Armstrong,Cassidy,Novelli,Tchorzewska,Jaxa-Chamiec,Dolle,Hallam,Leigh,Merritt,Moores,Rink
, p. 595 - 602 (2007/10/02)
Receptor mediated calcium entry (RMCE) is a now recognised mechanism by which the influx of Ca2+ into cells can occur. Agents which antagonise or block this mechanism are expected to possess anti-platelet aggregation and anti-inflammatory activities. The first series of RMCE blockers based upon the lead compound SC 38249, has been prepared. Their synthesis, activity against ADP evoked Ca2+ signals in human platelets and their anti-platelet aggregation activity is described. A trend between the c log P of these compounds and their activity as inhibitors of Ca2+ influx into human platelets stimulated by ADP was observed. This SAR study led to a 40-fold increase in activity over the initial lead compound.
