Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 50, Issue -, Pages 255-263Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.01.059
Keywords
1,4-Benzoxazine; Thrombin inhibitor; Fibrinogen receptor antagonists; Platelet aggregation; Designed dual ligands
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Funding
- Slovenian Research Agency [P1-0208]
- Ad Futura Foundation
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Fluorinated 3,4-dihydro-2H-1,4-benzoxazine derivatives possessing both thrombin inhibitory and glycoprotein IIb/IIIa receptor antagonistic activities were prepared as potential dual antithrombotic compounds. Fluorine scan (3-fluorobenzyl, 4-fluorobenzyl, 3,4-difluorobenzyl and 3,5-difluorobenzyl substituted compounds) was performed in order to obtain 6-(carboxymethyl)(3,4-difluorobenzyl) amino compound (9i) as the most potent compound with balanced dual activity (K-i(Thr) = 0.33 +/- 0.07 mu M, IC50(GP IIb/IIIa) = 1.1 +/- 0.6 mu M). (C) 2012 Elsevier Masson SAS. All rights reserved.
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