Warning: Undefined array key "mm" in /www/wwwroot/www.ai-bt.com/si.php on line 10 Deprecated: trim(): Passing null to parameter #1 ($string) of type string is deprecated in /www/wwwroot/www.ai-bt.com/si.php on line 10 Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.

Literature DB >> 18447380

Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.

Samuel Chackalamannil¹, Yuguang Wang, William J Greenlee, Zhiyong Hu, Yan Xia, Ho-Sam Ahn, George Boykow, Yunsheng Hsieh, Jairam Palamanda, Jacqueline Agans-Fantuzzi, Stan Kurowski, Michael Graziano, Madhu Chintala.

Abstract

The discovery of an exceptionally potent series of thrombin receptor (PAR-1) antagonists based on the natural product himbacine is described. Optimization of this series has led to the discovery of 4 (SCH 530348), a potent, oral antiplatelet agent that is currently undergoing Phase-III clinical trials for acute coronary syndrome (unstable angina/non-ST segment elevation myocardial infarction) and secondary prevention of cardiovascular events in high-risk patients.

Entities: Chemical Disease Gene Species

Mesh：

Substances：

Year: 2008 PMID： 18447380 DOI： 10.1021/jm800180e

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

Keyword Cloud
Cited

63 in total

1. Pharmacodynamics and pharmacokinetics of the novel PAR-1 antagonist vorapaxar (formerly SCH 530348) in healthy subjects.

Authors: Teddy Kosoglou; Larisa Reyderman; Renger G Tiessen; André A van Vliet; Robert R Fales; Robert Keller; Bo Yang; David L Cutler
Journal: Eur J Clin Pharmacol Date: 2011-09-21 Impact factor: 2.953

Review 2. Targeting proteinase-activated receptors: therapeutic potential and challenges.

Authors: Rithwik Ramachandran; Farshid Noorbakhsh; Kathryn Defea; Morley D Hollenberg
Journal: Nat Rev Drug Discov Date: 2012-01-03 Impact factor: 84.694

Review 3. New antithrombotic drugs: Antithrombotic Therapy and Prevention of Thrombosis, 9th ed: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines.

Authors: Jeffrey I Weitz; John W Eikelboom; Meyer Michel Samama
Journal: Chest Date: 2012-02 Impact factor: 9.410

Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.

1. Pharmacodynamics and pharmacokinetics of the novel PAR-1 antagonist vorapaxar (formerly SCH 530348) in healthy subjects.

Review 2. Targeting proteinase-activated receptors: therapeutic potential and challenges.

Review 3. New antithrombotic drugs: Antithrombotic Therapy and Prevention of Thrombosis, 9th ed: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines.

4. Vorapaxar: targeting a novel antiplatelet pathway.

Review 5. Signal transduction by protease-activated receptors.

Review 6. A review of antiplatelet drugs, coronary artery diseases and cardiopulmonary bypass.

Review 7. Recent Insights Into the Regulation of Coagulation and Thrombosis.

8. Total synthesis of the Galbulimima alkaloid (-)-GB17.

Review 9. Biased signalling and proteinase-activated receptors (PARs): targeting inflammatory disease.

Review 10. Role of the blood coagulation cascade in hepatic fibrosis.