SYNTHESIS OF DL-CIS- AND NYL)-AMINOMETHYL-1,3-DIOXOLAN-5-YL]-5(Z)-HEPTENOIC ACID ANALOGS AS PLATELET THROMBOXANE A(2) RECEPTOR ANTAGONISTS

Citation
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
Citations number
24
Categorie Soggetti
Chemistry Medicinal
ISSN journal
02235234
Volume
30
Issue
4
Year of publication
1995
Pages
321 - 326
Database
ISI
SICI code
0223-5234(1995)30:4<321:SODAN>2.0.ZU;2-L
Abstract
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).