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Antagonists of Vitamin K—Popular Coumarin Drugs and New Synthetic and Natural Coumarin Derivatives

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Department of Cosmetic Raw Materials Chemistry, Faculty of Pharmacy, Medical University of Lodz, Muszynskiego 1, 90-151 Łódź, Poland
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Department of General Biochemistry, Faculty of Biology and Environmental Protection, University of Lodz, Pomorska 141/143, 90-236 Łódź, Poland
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Department of Medical Pharmacy, Faculty of Pharmacy, Medical University of Lodz, Muszynskiego 1, 90-151 Łódź, Poland
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Centre of Molecular and Macromolecular Studies, Polish Academy of Sciences, Department of Bioorganic Chemistry, Sienkiewicza 112, 90-363 Łódź, Poland
*
Author to whom correspondence should be addressed.
Academic Editor: Konstantinos E. Litinas
Molecules 2020, 25(6), 1465; https://doi.org/10.3390/molecules25061465 (registering DOI)
Received: 18 December 2019 / Revised: 17 March 2020 / Accepted: 20 March 2020 / Published: 24 March 2020
(This article belongs to the Special Issue Synthesis and Bioactivity of Coumarin and Coumarin Derivatives)
Many natural coumarins and their chemically synthesized analogs and derivatives exert diverse properties, such as anticancer, antioxidant, anti-inflammatory, or anticoagulant, with the latter being of the utmost importance. The widely used warfarin, acenocoumarol, and phenprocoumon exert anticoagulant properties by inhibiting the vitamin K epoxide reductase complex. In this interdisciplinary review, we present biochemical principles of the coagulation processes and possible methods for their tuning based on the use of coumarins. We also summarize chemical methods of synthesis of coumarins and discuss structures and properties of those that have been used for a long time, as well as newly synthesized compounds. Brief information on the clinical use of coumarins and other anticoagulant drugs is given, including the severe effects of overdosing and methods for reversing their action. View Full-Text
Keywords: coumarins; coumarin derivatives; oral anticoagulants; cardiovascular diseases; vitamin K; vitamin K antagonists coumarins; coumarin derivatives; oral anticoagulants; cardiovascular diseases; vitamin K; vitamin K antagonists
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Kasperkiewicz, K.; Ponczek, M.B.; Owczarek, J.; Guga, P.; Budzisz, E. Antagonists of Vitamin K—Popular Coumarin Drugs and New Synthetic and Natural Coumarin Derivatives. Molecules 2020, 25, 1465.

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