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An overview of thrombin inhibitors in the perspective of structure-activity relationships.

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Thrombosis is one of the most important pathogenic factors that related to cardiovascular diseases. Presently, thrombin inhibitors have gradually gained prominence in clinical practice due to their unique potential, such… Click to show full abstract

Thrombosis is one of the most important pathogenic factors that related to cardiovascular diseases. Presently, thrombin inhibitors have gradually gained prominence in clinical practice due to their unique potential, such as dabigatran. Nevertheless, the risk of bleeding is not completely eliminated, and the threats of gastrointestinal bleeding are even increased in some cases. Therefore, it is urgent to develop new oral thrombin inhibitors with low side effects. In this paper, we summarized recent advances on the newly synthesized and isolated thrombin inhibitors from 2000 to 2019 and their structure-activity relationships (SARs) along with structure-dependent pharmacokinetic parameters, providing guidance for next generation of oral thrombin inhibitors.

Keywords: thrombin inhibitors; structure activity; structure; activity relationships

Journal Title: Current medicinal chemistry
Year Published: 2022

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