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Progress in the design of low molecular weight thrombin inhibitors
Author(s) -
Srivastava Stuti,
Goswami Lalit N.,
Dikshit Dinesh K.
Publication year - 2005
Publication title -
medicinal research reviews
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.868
H-Index - 130
eISSN - 1098-1128
pISSN - 0198-6325
DOI - 10.1002/med.20016
Subject(s) - antithrombotic , coagulation cascade , discovery and development of direct thrombin inhibitors , thrombin , medicine , coagulation , warfarin , low molecular weight heparin , thrombosis , pharmacology , heparin , anticoagulant , immunology , platelet , atrial fibrillation
Intravascular thrombosis and its complication, embolism, is a leading cause of morbidity and mortality throughout the world. Past few decades have seen a great deal of progress in the development of antithrombotic agents, though the current treatment options are limited to heparin, LMW heparins, and warfarin. Detailed understanding of the biochemical and biophysical mechanisms of activation and regulation of blood coagulation have helped in developing specific inhibitors of enzymes, especially thrombin, within the coagulation cascade. Thrombin plays a central role in the coagulation cascade and so has become the primary target for the development of antithrombotic drugs. The review covers the main pharmacological aspects of haemostasis and thrombosis and provides an update on low molecular weight thrombin inhibitors along with the limitations of the prevalent antithrombotic agents. Recent developments in small molecule inhibitors of Protease Activated Receptor‐1 (PAR‐1) which can be helpful for the treatment of thrombotic and vascular proliferative disorders, have also been discussed. © 2004 Wiley Periodicals, Inc.