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An Overview of Thrombin Inhibitors in the Perspective of Structureactivity Relationships

Jiangming Wang1, Xiaojing Sun1, Na Li1

  • 1College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, China.

Current Medicinal Chemistry
|September 6, 2022
PubMed

Insights

New oral thrombin inhibitors are crucial for cardiovascular disease treatment. This review summarizes recent advances in thrombin inhibitors, focusing on structure-activity relationships and pharmacokinetics to guide future drug development.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Thrombosis is a major risk factor for cardiovascular diseases.
  • Current thrombin inhibitors like dabigatran show potential but carry bleeding risks, especially gastrointestinal bleeding.
  • There is an urgent need for novel oral thrombin inhibitors with improved safety profiles.

Purpose of the Study:

  • To review recent advancements in synthesized and isolated thrombin inhibitors from 2000 to 2019.
  • To analyze structure-activity relationships (SARs) of these inhibitors.
  • To correlate structure with pharmacokinetic parameters to inform the development of next-generation oral thrombin inhibitors.

Main Methods:

  • Literature review of scientific publications from 2000 to 2019.
  • Analysis of structure-activity relationships (SARs) of identified thrombin inhibitors.
  • Evaluation of structure-dependent pharmacokinetic properties.

Main Results:

  • Identification and summary of newly developed oral thrombin inhibitors.
  • Detailed analysis of SARs for various inhibitor classes.
  • Correlation between molecular structure and pharmacokinetic behavior, including absorption, distribution, metabolism, and excretion.

Conclusions:

  • Recent research has yielded promising novel oral thrombin inhibitors.
  • Understanding SARs and pharmacokinetic parameters is key to designing safer and more effective anticoagulants.
  • This review provides a foundation for developing next-generation thrombin inhibitors with reduced side effects.

Keywords:
Antithromboticpharmacokineticsstructure-activity relationshipthrombin inhibitor

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