European Journal of Medicinal Chemistry p. 595 - 602 (1990)
Update date:2022-08-02
Topics:
Howson
Armstrong
Cassidy
Novelli
Tchorzewska
Jaxa-Chamiec
Dolle
Hallam
Leigh
Merritt
Moores
Rink
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.
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Doi:10.1016/S0040-4020(01)96012-0
(1990)Doi:10.1016/0022-328X(90)85478-H
(1990)Doi:10.1002/anie.201101524
(2011)Doi:10.1021/jo00172a056
(1983)Doi:10.1055/s-1990-27095
(1990)Doi:10.1016/S0040-4020(01)87896-0
(1990)