SYNTHESIS OF DL-CIS- AND (4R,5R)-TRANS-7-[2,2-DIMETHYL-4-(PHENYLSULFONYL)-AMINOMETHYL-1,3-DIOXOLAN-5-YL]-5(Z)-HEPTENOIC ACID ANALOGS AS PLATELET THROMBOXANE A(2) RECEPTOR ANTAGONISTS

The title compounds have been synthesized and their in vitro thromboxane A(2) (TxA(2)) receptor antagonist activity evaluated. Both cis and trans isomers (1, 2) were shown to specifically inhibit submaximal human platelet aggregation induced by 225 nM U46619 in a dose-dependent manner with an IC50 o...

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Published inEuropean journal of medicinal chemistry Vol. 30; no. 4; pp. 321 - 326
Main Authors KOMIOTIS, D, PANANOOKOOLN, S, ZAW, K, DIETER, JP, LEBRETON, GC, VENTON, DL
Format Journal Article
LanguageEnglish
Published ISSY-LES-MOULINEAUX Elsevier 01.01.1995
Subjects
Chemistry, Medicinal
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Science & Technology
ALCOHOLS
A2
1,3-DIOXOLANE
INVITRO
THROMBOXANE A
PROSTAGLANDIN ENDOPEROXIDES
DERIVATIVES
RECEPTOR ANTAGONIST
PLATELET AGGREGATION
AGGREGATION
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Summary:The title compounds have been synthesized and their in vitro thromboxane A(2) (TxA(2)) receptor antagonist activity evaluated. Both cis and trans isomers (1, 2) were shown to specifically inhibit submaximal human platelet aggregation induced by 225 nM U46619 in a dose-dependent manner 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 mu(M).
ISSN:0223-5234
1768-3254
DOI:10.1016/0223-5234(96)88240-7