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KMID : 0043320140370030332
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Archives of Pharmacal Research
2014 Volume.37 No. 3 p.332 ~ p.339
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Synthesis of thioether derivatives of quinazoline-4-one-2-thione and evaluation of their antiplatelet aggregation activity
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Eskandariyan Zahra
Zadeh Marjan Esfahani
Tehrani Kamaleddin Haj Mohammad Ebrahim
Mashayekhi Vida
Kobarfard Farzad
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Abstract
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A series of 2-(arylmethylthio)-3-phenylquinazolin-4-one derivatives have been synthesized and their antiplatelet aggregation activities were assessed against ADP and arachidonic acid-induced platelet aggregation in human plasma. Among the tested thioethers, derivative 2, 3, 5 and 16 were the most potent compounds with satisfactory IC50 for inhibition of platelet aggregation induced by ADP. Analysis of global physicochemical parameters shows some correlations between activities and molecular volume and also surface area of the studied derivatives.
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KEYWORD
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2-(Arylmethylthio)-3-phenylquinazolin-4-one, Antiplatelet aggregation, Thioether, Structure?activity relationship, Adenosine diphosphate, Arachidonic acid
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