Design, synthesis of novel tryptophan derivatives for antiplatelet aggregation activity based on tripeptide pENW (pGlu-Asn-Trp)
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- 作者：Zhouling Xiea ; Sen Fenga ; Ying Wangb ; Chen Caoa ; Jing Huanga ; Yahui Chenb ; Yi Kongb ; yikong668@163.com" class="auth_mail" title="E-mail the corresponding author ; Zhiyu Lia ; zhiyuli@cpu.edu.cn" class="auth_mail" title="E-mail the corresponding author
- 关键词：pENW ; Antiplatelet aggregation ; GPIIb/IIIa receptor inhibitor ; Tryptophan derivatives ; Bleeding risk
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2015
- 出版时间：18 September 2015
- 年：2015
- 卷：102
- 期：Complete
- 页码：363-374
- 全文大小：1619 K
文摘
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The small molecule compound 70 was identified based on the three mer peptide pENW (pGlu-Asn-Trp).
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A series of Trp derivatives were synthesized and evaluated for antiplatelet aggregation activity.
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The most potent compound 87 in our paper shows comparable ability as Tirofiban in inhibiting platelet aggregation.
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Compound 87 has less bleeding risk compared with Tirofiban.