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    Scientists Double Effectiveness of Anti-Inflammatory Drugs Synthesis

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    Scientists at Tyumen State University (UNTM), together with their colleagues from Omsk and Kokshetau in Kazakhstan, have developed an effective method to synthesise anti-inflammatory compounds that can be used in drugs. The findings were published in Chemistry of Heterocyclic Compounds magazine.

    Today, medicine is constantly in need of new drugs, that have higher pharmacological activity, are less toxic and have no negative side effects. The synthesis and study of the bioactivity of new organic molecules are also necessary, since there’s the phenomenon of addiction, as well as resistance to many modern drugs.

    Nonsteroidal compounds with anti-inflammatory activity based on oxazole-pyridine derivatives occupy a special place in modern medicine. It’s known that they not only have anti-inflammatory and analgesic, but also antibacterial and antitumor activity.

    However, modern methods to synthesise organic compounds based on oxazole-pyridine derivatives give a low reaction yield. In addition, by-products are formed during the reaction, which complicates the process of obtaining the desired compound.

    The authors of the study have proposed a new method to synthesise the 5-methyl-7-phenyl-2-(chloromethyl) oxazole [5,4-b] pyridine anti-inflammatory compound. According to the classical scheme, the chemical yield is about 20%. The researchers have managed to conduct a synthesis reaction with a chemical yield of 38-51%.

    “Based on laboratory-available organic compounds with the basic structure of a pyridine (or pyridone) molecule, we want to carry out chemical modifications in order to obtain new compounds with high biological activity, which could be used as medicines”, Irina Palamarchuk, the research engineer of the chromatography and spectroscopy department of UTMN, told Sputnik.

    The research team used classical methods and techniques of fine organic synthesis. In the future, the researchers plan to continue targeted modification with the introduction of pharmacophore groups; they also plan to study the “structure - biological activity” relations of new pyridine derivatives.

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