Thieno[2,3-b]pyridine derivatives are potent anti-platelet drugs, inhibiting platelet activation, aggregation and showing synergy with aspirin

Binsaleh, NK, Wigley, CA, Vagg-Whitehead, Kathryn, van Rensburg, M, Reynisson, J, Pilkington, LI, Barker, D, Jones, Sarah and Dempsey-Hibbert, N (2018) Thieno[2,3-b]pyridine derivatives are potent anti-platelet drugs, inhibiting platelet activation, aggregation and showing synergy with aspirin. European Journal of Medicinal Chemistry, 143. pp. 1997-2004. ISSN 1768-3254

Preview

Accepted Version
Available under License Creative Commons Attribution Non-commercial No Derivatives.
Download (878kB) | Preview

Official URL: https://www.sciencedirect.com/science/article/pii/...

Abstract

Drugs which inhibit platelet function are commonly used to prevent blood clot formation in patients with Acute Coronary Syndromes (ACS) or those at risk of stroke. The thieno[3,2-c]pyridine class of therapeutic agents, of which clopidogrel is the most commonly used, target the P2Y12 receptor, and are often used in combination with acetylsalicylic acid (ASA). Six thieno[2,3-b]pyridine were assessed for in vitro anti-platelet activity; all derivatives showed effects on both platelet activation and aggregation, and showed synergy with ASA. Some compounds demonstrated greater activity when compared to clopidogrel. These compounds, therefore, represent potential novel P2Y12 inhibitors for improved treatment for patients.

Item Type:	Article
Peer-reviewed:	Yes
Date Deposited:	09 Nov 2017 09:18
Publisher:	Elsevier
Additional Information:	This is an Author Accepted Manuscript of a paper accepted for publication in European Journal of Medicinal Chemistry, published by and copyright Elsevier.
Divisions:	Faculties > Science and Engineering
Subject terms:	Science & Technology, Life Sciences & Biomedicine, Chemistry, Medicinal, Pharmacology & Pharmacy, Thienopyridine, Platelets, Thrombosis, Clopidogrel, Aspirin, ACUTE CORONARY SYNDROMES, ACUTE MYOCARDIAL-INFARCTION/, TYPE-2 DIABETES-MELLITUS, IN-VITRO, P2Y(12) RECEPTOR, ARTERY-DISEASE, P-SELECTIN, CLOPIDOGREL, PRASUGREL, TRIAL, Humans, Aspirin, Pyridines, Platelet Aggregation Inhibitors, Molecular Structure, Structure-Activity Relationship, Platelet Activation, Platelet Aggregation, Dose-Response Relationship, Drug, Adult, Female, Male, Young Adult, Aspirin, Clopidogrel, Platelets, Thienopyridine, Thrombosis, Adult, Aspirin, Dose-Response Relationship, Drug, Female, Humans, Male, Molecular Structure, Platelet Activation, Platelet Aggregation, Platelet Aggregation Inhibitors, Pyridines, Structure-Activity Relationship, Young Adult, 0304 Medicinal And Biomolecular Chemistry, 1115 Pharmacology And Pharmaceutical Sciences, 0305 Organic Chemistry, Medicinal & Biomolecular Chemistry
URI:	https://e-space.mmu.ac.uk/id/eprint/619400
DOI:	https://doi.org/10.1016/j.ejmech.2017.11.014
ISSN	1768-3254

Impact and Reach

Statistics

DownloadsShow export options

Activity Overview

6 month trend

752Downloads

6 month trend

509Hits

Additional statistics for this dataset are available via IRStats2.

Altmetric

Repository staff only

Edit record