Metabolism-based synthesis, biologic evaluation and SARs analysis of O-methylated analogs of quercetin as thrombin inhibitors

ZH Shi, NG Li, YP Tang, JP Yang, JA Duan

Index: Shi, Zhi-Hao; Li, Nian-Guang; Tang, Yu-Ping; Wei-Li; Lian-Yin; Yang, Jian-Ping; Hao-Tang; Duan, Jin-Ao European Journal of Medicinal Chemistry, 2012 , vol. 54, p. 210 - 222

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Citation Number: 27

Abstract

In blood, quercetin is mainly found in metabolized forms. In order to study the activities of these quercetin metabolites in cardiovascular disease, 17 methylquercetin derivatives were synthesized based on metabolism in vivo, their thrombin inhibition activity were evaluated through the analyzation of prothrombin time (PT), activated partial thromboplastin time (APTT), thrombin time (TT) and fibrinogen (FIB). The results showed that 6 ...