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4-(Het)aryl-4,7-dihydroazolopyrimidines and Their Tuberculostatic Activity

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Abstract

Structural analogs of a promising antituberculous agent, ethyl 5-methyl-7-(thiophen-2-yl)-4,7-dihydro[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxylate have been synthesized by three-component condensations of various aromatic or hetaromatic aldehydes with several β-dicarbonyl compounds (CH acids) and 1H-1,2,4-triazol-5-amine or 1H-pyrazol-5-amine. The obtained compounds have been evaluated for tuberculostatic activity, and structure-activity relations have been analyzed.

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Acknowledgments

The authors thank the Ural Research Institute of Phthisiopulmonology (Yekaterinburg) for performing biological studies in vitro.

Funding

This study was performed under financial support by the Russian Science Foundation (project no. 15-13-00077-P).

Author information

Authors and Affiliations

  1. Postovskii Institute of Organic Synthesis, Ural Branch, Russian Academy of Sciences, Yekaterinburg, Russia

    Yu. A. Titova, E. S. Filatova, O. V. Fedorova, G. L. Rusinov & V. N. Charushin

  2. Yeltsin Ural Federal University, Yekaterinburg, Russia

    Yu. A. Titova, G. L. Rusinov & V. N. Charushin

Authors
  1. Yu. A. Titova
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  2. E. S. Filatova
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  3. O. V. Fedorova
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  4. G. L. Rusinov
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  5. V. N. Charushin
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Corresponding author

Correspondence to Yu. A. Titova.

Additional information

Dedicated to Full Member of the Russian Academy of Sciences O.N. Chupakhin on his 85th anniversary

Russian Text© The Author(s), 2019, published in Zhurnal Organicheskoi Khimii, 2019, Vol. 55, No. 6, pp. 871–878.

Conflict of Interests

The authors declare no conflict of interests.

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Titova, Y.A., Filatova, E.S., Fedorova, O.V. et al. 4-(Het)aryl-4,7-dihydroazolopyrimidines and Their Tuberculostatic Activity. Russ J Org Chem 55, 775–781 (2019). https://doi.org/10.1134/S107042801906006X

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  • DOI: https://doi.org/10.1134/S107042801906006X

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