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Towards dual antithrombotic compounds - Balancing thrombin inhibitory and fibrinogen GPIIb/IIIa binding inhibitory activities of 2,3-dihydro-1,4-benzodioxine derivatives through regio- and stereoisomerism
Ilić, Miloš (Avtor), Dunkel, Petra (Avtor), Ilaš, Janez (Avtor), Chabielska, Ewa (Avtor), Zakrzeska, Agnieszka (Avtor), Mátyus, Péter (Avtor), Kikelj, Danijel (Avtor)

URLURL - Predstavitvena datoteka, za dostop obiščite http://www.sciencedirect.com/science/article/pii/S022352341300010X# Novo okno

Izvleček
Enantiomers of 2,3-dihydro-1,4-benzodioxine derivatives possessing both thrombin and fibrinogen GPIIb/IIIa binding inhibitory activities were preparedfrom (R)- and (S)-glycidol as potential dual antithrombotic compounds.The influence of chirality and substitution pattern on thrombin inhibition and on inhibition of fibrinogen binding to GPIIb/IIIa was analyzed.Docking studies were used in an attempt to rationalize the results. The (S)-isomers of both 2,3-dihydro-1,4-benzodioxine regioisomers at positions 6 and 7 were found to be better thrombin inhibitors than the corresponding (R)-enantiomers, whereas we observed that stereochemistry does not display a consistent influence on fibrinogen GPIIb/ IIIa binding inhibitory activity. Compound 11b, the (S)-isomer of the 6-substituted regioisomer, possessed the best balanced dual activity, with Ki(thrombin) = 1.67 0.27 mM and IC50(GPIIb/IIIa) = 0.665 0.26 mM, raising the hope that merging anticoagulant and platelet antiaggregatory activities in the same molecule could lead to successful multitarget antithrombotic agents.

Jezik:Angleški jezik
Ključne besede:antithrombotic thrombin inhibitor, GPIIb/IIIa 2, 3-dihydro-1, 4-benzodioxine, dual antithrombotic compound, multitarget
Vrsta gradiva:Delo ni kategorizirano (r6)
Tipologija:1.01 - Izvirni znanstveni članek
Organizacija:FFA - Fakulteta za farmacijo
Leto izida:2013
Št. strani:str. 329-340
Številčenje:Vol. 62
UDK:542+543:615.221
ISSN pri članku:0223-5234
DOI:10.1016/j.ejmech.2013.01.002 Povezava se odpre v novem oknu
COBISS.SI-ID:3391601 Povezava se odpre v novem oknu
Število ogledov:437
Število prenosov:120
Metapodatki:XML RDF-CHPDL DC-XML DC-RDF
 
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Gradivo je del revije

Naslov:European journal of medicinal chemistry
Skrajšan naslov:Eur. j. med. chem.
Založnik:Elsevier
ISSN:0223-5234
COBISS.SI-ID:25429760 Novo okno

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