The most effective
Chemists from Russia have created a safe medicine for blood thinning
Scientists from The Institute of Organic Chemistry of the Russian Academy of Sciences has created a new method for the synthesis of warfarin, a blood thinning drug that allows you to obtain safe and at the same time effective doses of this drug, according to an article published in the journal Green Chemistry.
"If you learn to get exactly this isomer of warfarin, then the dose of the drug can be reduced by five times. And why swallow more of it, if less is possible? Accordingly, the risks of all kinds of overdoses will decrease," said Alexander Kucherenko, senior researcher at the Institute of Organic Chemistry of the Russian Academy of Sciences, whose words are quoted by the RNF press service.
Warfarin is one of the drugs that can dissolve blood clots and dilute blood. It was accidentally discovered in the 1920s on farms in the USA after a mysterious epidemic of the death of cattle that ate fresh hay. Subsequently, it was used as rat poison, and only in the early 1950s it began to be used for medical purposes after an unsuccessful suicide attempt. Since then, it has remained one of the essential medicines.
Like many other organic molecules, warfarin has two different forms related to how the tails of its molecules are "rotated" relative to each other. They have the same physical and chemical properties, but at the same time they act differently on the body, since many enzymes in our cells are "tuned" to work with only one type of such molecules.
For example, there are two variations of warfarin, s-warfarin and r-warfarin.
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The first one acts about five times stronger than the second one for the reason that it better suppresses the work of enzymes responsible for the synthesis of vitamin K. This creates difficulties in determining the dosage of the drug, since warfarin is produced as a mixture of s- and r-molecules, whose proportion is not always constant and known in advance.
Russian chemists eliminated this problem by opening chains of reactions that make it possible to obtain either only s-warfarin or r-warfarin. To do this, they returned to the past and studied how coumarin, a substance with the smell of freshly mown grass, interacts with various organic substances and turns into a "cattle killer", the culprit of the mysterious case of cows in the 1920s.
The essence of their idea was very simple – scientists expected that organic catalysts, like other substances inside the body, would interact with only one of the two coumarin variants, turned in the "right" direction, and produce warfarin molecules of only one type.
As it turned out, there is a whole set of similar molecules, different variations of compounds of ammonia and isoquinoline, an aromatic hydrocarbon, which work in a similar way. The best versions of them produce almost pure warfarin of one type or another. Only 1% of the molecules, as shown by the experiments of Russian chemists, were turned in the "wrong" direction.
In the future, as Kucherenko and his colleagues note, it will be possible to receive not only warfarin, but also many other drugs, such as levomycetin, rolipram and paroxetine.
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