Abstract
Novel structural analogs of isothiobarbamine, which differ from the prototype scaffold by the substituent at position 2 of the pyrimidine heterocycle, were for the first time synthesized and characterized. Data acquired in pharmacological experiments in vivo revealed that compounds 1b—d and 10 increase physical productivity, whereas compounds 1c and 10 exhibit a nootropic effect, compound 8a shows a psychostimulating effect, and compound 1b exhibits anxiolytic properties. The results reported herein indicate that the drug discovery based on new structural analogs of isothiobarbamine is promising since it may lead to drugs for the prevention and treatment of asthenia (chronic fatigue syndrome).
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Funding
This work was financially supported by the Russian Science Foundation (Project No. 19-13-00123) and was carried out using analytical instruments of the Center for Collective Use (CCU) at the N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry of the Siberian Branch of the Russian Academy of Sciences.
All the experiments involving animals were carried out according to the legislation and technical standards of the Eurasian Economic Union on appropriate laboratory practice (GOST 53434-2019 and GOST D 51000.4-2011), Directive 2010/63/EU of the European Parliament and the Council of the European Union, and the interstate standard (GOST 33044-2014). The research protocol was approved by the local ethics committee (Regional Research Ethics Committee of the Volgograd Region, IRB 00005839 IORG 0004900 (OHRP)) on January 29, 2021 (No. 2021/003).
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Dedicated to Academician of the Russian Academy of Sciences O. M. Nefedov on the occasion of his 90th birthday.
Published in Russian in Izyestiya AkademiiNauk. Seriya Khimicheskaya, No. 11, pp. 2220–2226, November, 2021.
The authors declare no competing interests.
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Novakov, I.A., Sheikin, D.S., Ruchko, E.A. et al. Synthesis and biological properties of novel structural analogs of isothiobarbamine. Russ Chem Bull 70, 2220–2226 (2021). https://doi.org/10.1007/s11172-021-3336-7
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DOI: https://doi.org/10.1007/s11172-021-3336-7