D. Komiotis et al., SYNTHESIS OF DL-CIS- AND NYL)-AMINOMETHYL-1,3-DIOXOLAN-5-YL]-5(Z)-HEPTENOIC ACID ANALOGS AS PLATELET THROMBOXANE A(2) RECEPTOR ANTAGONISTS, European journal of medicinal chemistry, 30(4), 1995, pp. 321-326
The title compounds have been synthesized and their in vitro thromboxa
ne A(2) (TxA(2)) receptor antagonist activity evaluated. Both cis and
trans isomers (1, 2) were shown to specifically inhibit submaximal hum
an platelet aggregation induced by 225 nM U46619 in a dose-dependent m
anner with an IC50 of 1 mu M. The concentration of 1 and 2 required to
completely block maximal aggregation induced by 3 mu M U46619 was 3 m
u(M).