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Molecules 2015, 20(6), 11046-11062; doi:10.3390/molecules200611046

Development of Orally Active Thrombin Inhibitors for the Treatment of Thrombotic Disorder Diseases

Department of Medicinal Chemistry, Nanjing University of Chinese Medicine, Nanjing 210023, China
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Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 14 May 2015 / Accepted: 10 June 2015 / Published: 15 June 2015
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [916 KB, uploaded 15 June 2015]   |  

Abstract

Thrombotic disorders represent the major share of the various cardiovascular diseases, and significant progress has been made in the development of synthetic thrombin inhibitors as new anticoagulants. In addition to the development of highly potent and selective inhibitors with improved safety and suitable half-life, several allosteric inhibitors have been designed and synthesized, that did not fully nullify the procoagulant signal and thus could result in reduced bleeding complications. Furthermore, natural products with thrombin inhibitory activity have been isolated, and some natural products have been modified in order to improve their inhibitory activity and metabolic stability. This review summarizes the development of orally active thrombin inhibitors for the treatment of thrombotic disorder diseases, which could serve as a reference for the interested researchers. View Full-Text
Keywords: thrombin; thrombotic disorders; allosteric inhibitors; natural products; orally active; coagulation; thrombosis thrombin; thrombotic disorders; allosteric inhibitors; natural products; orally active; coagulation; thrombosis
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

He, L.-W.; Dai, W.-C.; Li, N.-G. Development of Orally Active Thrombin Inhibitors for the Treatment of Thrombotic Disorder Diseases. Molecules 2015, 20, 11046-11062.

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