Design, synthesis and evaluation of novel 2-amino-3-(naphth-2-yl)propanoic acid derivatives as potent inhibitors of platelet aggregation | Health & Environmental Research Online (HERO)

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HERO ID

3453173

Reference Type

Journal Article

Title

Design, synthesis and evaluation of novel 2-amino-3-(naphth-2-yl)propanoic acid derivatives as potent inhibitors of platelet aggregation

Author(s)

Xie, Z; Oscar, B; Zhao, L; Ding, X; Cao, C; Feng, S; Li, H; Pan, C; Bian, Z; Li, Y; Wang, W; Kong, Y; Li, Z

Year

2017

Is Peer Reviewed?

Yes

Journal

European Journal of Medicinal Chemistry
ISSN: 0223-5234
EISSN: 1768-3254

Volume

125

Page Numbers

197-209

Language

English

PMID

27662032

DOI

10.1016/j.ejmech.2016.09.032

Web of Science Id

WOS:000390496600013

URL

http://://WOS:000390496600013
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Abstract

Based upon LX2421, a previously identified antiplatelet aggregation agent, a series of novel 2-amino-3-(naphth-2-yl)propanoic acid derivatives were designed, synthesized and evaluated. Among them, compounds LX14 and LX25 were identified as promising antiplatelet aggregation agents. The in vitro biologic study demonstrated that LX14 can block platelet aggregation induced by four different inducers and displays comparable potency in inhibiting GPIIb/IIIa receptor in comparison with Tirofiban. In addition, LX14 has much lower risk of bleeding than Tirofiban and shows significant antithrombotic activity in vivo. Taking together, the results indicated that LX14 is a promising GPIIb/IIIa receptor antagonist against platelet aggregation worthy of further evaluation.

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