Synthesis of thioether derivatives of quinazoline-4-one-2-thione and evaluation of their antiplatelet aggregation activity

被引：0
|
作者：
Zahra Eskandariyan
Marjan Esfahani Zadeh
Kamaleddin Haj Mohammad Ebrahim Tehrani
Vida Mashayekhi
Farzad Kobarfard
机构：
[1] Shahid Beheshti University of Medical Sciences,Department of Medicinal Chemistry, School of Pharmacy
[2] Shahid Beheshti University of Medical Sciences,Phytochemistry Research Center
来源：
Archives of Pharmacal Research | 2014年 / 37卷
关键词：
2-(Arylmethylthio)-3-phenylquinazolin-4-one; Antiplatelet aggregation; Thioether; Structure–activity relationship; Adenosine diphosphate; Arachidonic acid;
D O I：
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中图分类号：
学科分类号：
摘要：
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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页码：332 / 339
页数：7
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