Email this article Synthesis and tuberculostatic activity of podands with a dihydropyrimidine fragment
- Authors: Filatova E.S.1,2, Fedorova O.V.1,2, Titova Y.A.1,2, Slepukhin P.A.2, Kravchenko M.A.3, Skornyakov S.N.3, Rusinov G.L.1,2, Charushin V.N.1,2
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Affiliations:
- Ural Federal University named after the first President of Russia B. N. Yeltsin
- I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences
- Ural Research Institute of Phthisiopulmonology, Russian Ministry of Healthcare
- Issue: Vol 65, No 5 (2016)
- Pages: 1360-1364
- Section: Full Articles
- URL: https://journals.rcsi.science/1066-5285/article/view/238306
- DOI: https://doi.org/10.1007/s11172-016-1462-4
- ID: 238306
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Abstract
A method for the preparation of 3-oxobutanoate-containing podands differing in the length of the polyether fragment by acetoacetylation of oligo(ethylene glycols) with 2,2,6-trimethyl-4H-1,3-dioxin-4-one upon heating in toluene was optimized. A multi-component Biginelli reaction was used for the formation of the dihydropyrimidine ring on the ether matrix obtained. Tuberculostatic activity of dihydropyrimidine podands in the in vitro experiments against a laboratory strain H37Rv was studied. A combination of dihydropyrimidine and podand fragments imparts tuberculostatic activity to the compounds obtained, which noticeably enhances with the increase in the oxyethylene spacer length.
About the authors
E. S. Filatova
Ural Federal University named after the first President of Russia B. N. Yeltsin; I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences
Author for correspondence.
Email: sintonin@mail.ru
Russian Federation, 19 ul. Mira, Ekaterinburg, 620002; 22 ul. S. Kovalevskoi, Ekaterinburg, 620219
O. V. Fedorova
Ural Federal University named after the first President of Russia B. N. Yeltsin; I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences
Email: sintonin@mail.ru
Russian Federation, 19 ul. Mira, Ekaterinburg, 620002; 22 ul. S. Kovalevskoi, Ekaterinburg, 620219
Yu. A. Titova
Ural Federal University named after the first President of Russia B. N. Yeltsin; I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences
Email: sintonin@mail.ru
Russian Federation, 19 ul. Mira, Ekaterinburg, 620002; 22 ul. S. Kovalevskoi, Ekaterinburg, 620219
P. A. Slepukhin
I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences
Email: sintonin@mail.ru
Russian Federation, 22 ul. S. Kovalevskoi, Ekaterinburg, 620219
M. A. Kravchenko
Ural Research Institute of Phthisiopulmonology, Russian Ministry of Healthcare
Email: sintonin@mail.ru
Russian Federation, 50 ul. XXII parts´ezda, Ekaterinburg, 620039
S. N. Skornyakov
Ural Research Institute of Phthisiopulmonology, Russian Ministry of Healthcare
Email: sintonin@mail.ru
Russian Federation, 50 ul. XXII parts´ezda, Ekaterinburg, 620039
G. L. Rusinov
Ural Federal University named after the first President of Russia B. N. Yeltsin; I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences
Email: sintonin@mail.ru
Russian Federation, 19 ul. Mira, Ekaterinburg, 620002; 22 ul. S. Kovalevskoi, Ekaterinburg, 620219
V. N. Charushin
Ural Federal University named after the first President of Russia B. N. Yeltsin; I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences
Email: sintonin@mail.ru
Russian Federation, 19 ul. Mira, Ekaterinburg, 620002; 22 ul. S. Kovalevskoi, Ekaterinburg, 620219
