Ural Research Institute for Phthisiopulmonology

Yekaterinburg, Russia

Ural Research Institute for Phthisiopulmonology

Yekaterinburg, Russia
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Garifullin B.F.,RAS Arbuzov Institute of Organic and Physical Chemistry | Sharipova R.R.,RAS Arbuzov Institute of Organic and Physical Chemistry | Strobykina I.Yu.,RAS Arbuzov Institute of Organic and Physical Chemistry | Andreeva O.V.,RAS Arbuzov Institute of Organic and Physical Chemistry | And 2 more authors.
Russian Journal of Organic Chemistry | Year: 2015

Macrocyclic glycoterpenoids containing trehalose and isosteviol fragments have been synthesized. Selective screening has revealed compounds exhibiting antitubercular activity against H37RV, M. Avium and M. Terrae at a level comparable to the known antitubercular drugs isoniazid, ofloxacin, and pyrazinamide. © 2015 Pleiades Publishing, Ltd.


Izmest'ev Y.,RAS Arbuzov Institute of Organic and Physical Chemistry | Andreeva O.,RAS Arbuzov Institute of Organic and Physical Chemistry | Sharipova R.,RAS Arbuzov Institute of Organic and Physical Chemistry | Garifullin B.,RAS Arbuzov Institute of Organic and Physical Chemistry | And 3 more authors.
Phosphorus, Sulfur and Silicon and the Related Elements | Year: 2016

Several phosphorus containing glycolipids on the basis of glucuronic acid have been synthesized. The target compounds inhibited the in vitro growth of M. tuberculosis at MIC values of 12.5 μg/mL. © 2016 Taylor & Francis Group, LLC.


Verbitskiy E.V.,Ural Federal University | Baskakova S.A.,Russian Academy of Sciences | Kravchenko M.A.,Ural Research Institute for Phthisiopulmonology | Skornyakov S.N.,Ural Research Institute for Phthisiopulmonology | And 3 more authors.
Bioorganic and Medicinal Chemistry | Year: 2016

Various 5-(fluoroaryl)-4-(hetero)aryl substituted pyrimidines have been synthesized based on the Suzuki cross-coupling and nucleophilic aromatic substitution of hydrogen (SN H) reactions starting from commercially available 5-bromopyrimidine and their antitubercular activity against Mycobacterium tuberculosis H37Rv has been explored. The outcome of the study disclose that, some of the compounds have showed promising activity in micromolar concentration against Mycobacterium tuberculosis H37Rv, Mycobacterium avium, Mycobacterium terrae, and multidrug-resistant strains isolated from tuberculosis patients in Ural region (Russia). The data concerning the ‘structure–activity’ relationship for fluorinated compounds have been discussed. © 2016 Elsevier Ltd


Verbitskiy E.V.,Ural Federal University | Toporova M.S.,Russian Academy of Sciences | Kodess M.I.,Russian Academy of Sciences | Ezhikova M.A.,Russian Academy of Sciences | And 7 more authors.
Arkivoc | Year: 2014

The Petasis reaction of 6-alkoxy adducts of 1-alkyl-2,3-dicyano-5- arylpyrazinium salts with aromatic boronic acids, such as 2-thienylboronic, 2-furanylboronic and 3-thienylboronic acids, or their benzo analogs in dichloromethane proceeds smoothly at room temperature with the formation of the corresponding 5-aryl-6-hetaryl substituted 1,6-dihydropyrazine derivatives. All dihydropyrazines were separated as pure enantiomers by chiral HPLC, and their absolute configurations for each pair of enantiomers have been determined by X-ray analysis. Individual enantiomers were screened in vitro for their antimycobacterial activities against Mycobacterium tuberculosis H37Rv, avium, terrae and extensively drug-resistant and multi-drug-resistant strains isolated from tuberculosis patients in Ural region (Russia). It has been shown that several compounds exhibit a good level of antituberculosis activity compared to the reference drugs. © ARKAT-USA, Inc.


Kravchenko M.A.,Ural Research Institute for Phthisiopulmonology | Verbitskiy E.V.,Ural Federal University | Skornyakov S.N.,Ural Research Institute for Phthisiopulmonology | Slepukhin P.A.,Ural Federal University | And 3 more authors.
Anti-Infective Agents | Year: 2016

A simple method based on hydrolysis of 2,3-dicyanopyrazinium salts has been used for the synthesis of the corresponding 5-(hetero)aryl-3-cyano-1-ethyl-2(1H)-pyrazinones. Also, the series of novel 1-ethyl-5-(hetero)aryl-1,6-dihydropyrazine-2,3-dicarbonitriles have been obtained through reduction of the same pyrazinium salts with triethylsilane. The obtained compounds proved to be active in micromolar concentrations in vitro against Mycobacterium tuberculosis H37Rv, Mycobacterium avium, Mycobacterium terrae, as well as against rifampicin and isoniazid-resistance strains of Mycobacterium tuberculosis. The data for acute in vivo toxicity in mice have been obtained for these compounds which appear to be promising antitubercular agents. © 2016 Bentham Science Publishers.


Verbitskiy E.V.,Ural Federal University | Cheprakova E.M.,Ural Federal University | Slepukhin P.A.,Ural Federal University | Kravchenko M.A.,Ural Research Institute for Phthisiopulmonology | And 4 more authors.
European Journal of Medicinal Chemistry | Year: 2015

Abstract Combination of the Suzuki cross-coupling and nucleophilic aromatic substitution of hydrogen (SNH) reactions proved to be a convenient method for the synthesis of C(4) and/or C(5) mono(thienyl) and di(thienyl) substituted pyrimidines from commercially available 5-bromopyrimidine. All new pyrimidines were found to be active in micromolar concentrations in vitro against H37Rv, avium, terrae, rifampicin and isoniazid-resistance strains of Mycobacterium tuberculosis. The data for acute in vivo toxicity in mice have been obtained for these compounds which appear to be promising antitubercular agents. A series of C-4 and/or C-5 thienyl substituted pyrimidines were synthesized.All compounds were evaluated for their antimycobacterial activities. © 2015 Elsevier Masson SAS.


Verbitskiy E.V.,Ural Federal University | Slepukhin P.A.,Ural Federal University | Kravchenko M.A.,Ural Research Institute for Phthisiopulmonology | Skornyakov S.N.,Ural Research Institute for Phthisiopulmonology | And 6 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2015

The Petasis reaction of 6-hydroxy adducts of 1-alkyl-2,3-dicyano-5-arylpyrazinium salts with trans-styrylboronic acids proved to proceed smoothly at room temperature to give the corresponding 5-(hetero)aryl-6-styryl substituted 1,6-dihydropyrazine derivatives. Also it has been found that C(6) unsubstituted 1,6-dihydro- or 1,4,5,6-tetrahydropyrazine derivatives can be easy prepared in high yields from the corresponding pyrazinium salts by reduction with triethylsilane. All synthesized compounds were screened in vitro for their antifungal activities against seven pathogenic fungal strains and antimycobacterial activities against Mycobacterium tuberculosis H37Rv, avium, terrae and multi-drug-resistant strains isolated from tuberculosis patients in the Ural region (Russia). © 2014 Elsevier Ltd. All rights reserved.


Kravchenko M.A.,Ural Research Institute for Phthisiopulmonology | Verbitskiy E.V.,Ural Federal University | Medvinskiy I.D.,Ural Research Institute for Phthisiopulmonology | Rusinov G.L.,Ural Federal University | Charushin V.N.,Ural Federal University
Bioorganic and Medicinal Chemistry Letters | Year: 2014

Combination of the Suzuki cross-coupling and nucleophilic aromatic substitution of hydrogen (SN H) reactions proved to be a convenient method for the synthesis of 5-styryl-4-(hetero)aryl substituted pyrimidines from commercially available 5-bromopyrimidine. All intermediate 5-bromo-4-(hetero)aryl substituted pyrimidines and also the targeted 5-styryl-4-(hetero)arylpyrimidines were found to be active in micromolar concentrations in vitro against Mycobacterium tuberculosis H37Rv, avium, terrae, and multi-drug-resistant strain isolated from tuberculosis patients in Ural region (Russia). It has been found that some of these compounds possess a low toxicity and have a bacteriostatic effect, comparable and even higher with that of first-line antituberculosis drugs. © 2014 Elsevier Ltd. All rights reserved.


Cheprakova E.M.,Russian Academy of Sciences | Verbitskiy E.V.,Ural Federal University | Ezhikova M.A.,Russian Academy of Sciences | Kodess M.I.,Russian Academy of Sciences | And 7 more authors.
Russian Chemical Bulletin | Year: 2014

It has been shown that various combinations of nucleophilic aromatic substitution of hydrogen (SN H), SN ipso and the microwave-assisted Suzuki cross-coupling reactions are a versatile method for the synthesis of 5-(het)aryl-2-(thio)morpholinopyrimidine and 4,5-di(het)aryl-2-(thio)morpholinopyrimidine derivatives. All synthesized pyrimidines were found to be active in micromolar concentrations in vitro against Mycobacterium tuberculosis H37Rv. © 2014 Springer Science+Business Media New York.


PubMed | Russian Academy of Sciences and Ural Research Institute for Phthisiopulmonology
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2016

Synthetic routes to novel N-(purin-6-yl)- and N-(2-aminopurin-6-yl) conjugates with amino acids and glycine-containing dipeptides were developed. In vitro testing of 42 new and known compounds made it possible to reveal a series of N-(purin-6-yl)- and N-(2-aminopurin-6-yl) conjugates exhibiting significant antimycobacterial activity against Mycobacterium tuberculosis H37Rv, Mycobacterium avium, Mycobacterium terrae, and multidrug-resistant M. tuberculosis strain isolated from tuberculosis patients in the Ural region (Russia). N-(2-Aminopurin-6-yl)- and N-(purin-6-yl)-glycyl-(S)-glutamic acids were the most active compounds.

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