Fluorinated dual antithrombotic compounds based on 1,4-benzoxazine scaffold.

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Ilic M, Kikelj D, Ilas J

Fluorinated dual antithrombotic compounds based on 1,4-benzoxazine scaffold.

Eur J Med Chem. 2012 Apr;50:255-63. doi: 10.1016/j.ejmech.2012.01.059. Epub 2012 Feb 8.

PubMed ID

22365562 [ View in PubMed

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Abstract

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+/-0.07muM, IC(50(GP IIb/IIIa))=1.1+/-0.6muM).

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Tirofiban	Integrin beta-3	IC 50 (nM)	0.37	N/A	N/A	Details