Synthesis and tuberculostatic activity of podands with a dihydropyrimidine fragment


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Resumo

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.

Sobre autores

E. 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

Autor responsável pela correspondência
Email: sintonin@mail.ru
Rússia, 19 ul. Mira, Ekaterinburg, 620002; 22 ul. S. Kovalevskoi, Ekaterinburg, 620219

O. 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
Rússia, 19 ul. Mira, Ekaterinburg, 620002; 22 ul. S. Kovalevskoi, Ekaterinburg, 620219

Yu. 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
Rússia, 19 ul. Mira, Ekaterinburg, 620002; 22 ul. S. Kovalevskoi, Ekaterinburg, 620219

P. Slepukhin

I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences

Email: sintonin@mail.ru
Rússia, 22 ul. S. Kovalevskoi, Ekaterinburg, 620219

M. Kravchenko

Ural Research Institute of Phthisiopulmonology, Russian Ministry of Healthcare

Email: sintonin@mail.ru
Rússia, 50 ul. XXII parts´ezda, Ekaterinburg, 620039

S. Skornyakov

Ural Research Institute of Phthisiopulmonology, Russian Ministry of Healthcare

Email: sintonin@mail.ru
Rússia, 50 ul. XXII parts´ezda, Ekaterinburg, 620039

G. 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
Rússia, 19 ul. Mira, Ekaterinburg, 620002; 22 ul. S. Kovalevskoi, Ekaterinburg, 620219

V. 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
Rússia, 19 ul. Mira, Ekaterinburg, 620002; 22 ul. S. Kovalevskoi, Ekaterinburg, 620219


Declaração de direitos autorais © Springer Science+Business Media New York, 2016

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