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Matyugina E.,RAS Engelhardt Institute of Molecular Biology | Khandazhinskaya A.,RAS Engelhardt Institute of Molecular Biology | Chernousova L.,Central Tuberculosis Research Institute RAMS | Andreevskaya S.,Central Tuberculosis Research Institute RAMS | And 5 more authors.
Bioorganic and Medicinal Chemistry | Year: 2012

A series of new carbocyclic uracil derivatives were synthesized and evaluated as potential antituberculosis agents. Racemic 1-[4′-hydroxy- 2′-cyclopenten-1′-yl]-5-tetradecynyluracil completely inhibited the growth of Mycobacterium tuberculosis H37Rv in vitro at a concentration of 10 μg/ml. Individual (+) and (-) isomers of the above uracil derivative were isolated and showed the same level of activity against two strains of Mycobacterium tuberculosis: laboratory sensitive (H37Rv) and clinical resistant to five top antituberculosis drugs (MS-115). © 2012 Elsevier Ltd. All rights reserved. Source


Shmalenyuk E.R.,RAS Engelhardt Institute of Molecular Biology | Chernousova L.N.,Central Tuberculosis Research Institute RAMS | Karpenko I.L.,RAS Engelhardt Institute of Molecular Biology | Kochetkov S.N.,RAS Engelhardt Institute of Molecular Biology | And 5 more authors.
Bioorganic and Medicinal Chemistry | Year: 2013

Two sets of pyrimidine nucleoside derivatives bearing extended alkyloxymethyl or alkyltriazolidomethyl substituents at position 5 of the nucleobase were synthesized and evaluated as potential antituberculosis agents. The impact of modifications at 3′- and 5′-positions of the carbohydrate moiety on the antimycobacterial activity and cytotoxicity was studied. The highest effect was shown for 5-dodecyloxymethyl-2′- deoxyuridine, 5-decyltriazolidomethyl-2′-deoxyuridine, and 5-dodecyltriazolidomethyl-2′-deoxycytidine. They effectively inhibited the growth of two Mycobacterium tuberculosis strains in vitro, laboratory H37Rv (MIC99 = 20, 10, and 20 μg/mL, respectively) and clinical MDR MS-115 resistant to five top antituberculosis drugs (MIC99 = 50, 10, and 10 μg/mL, respectively). © 2013 Elsevier Ltd. All rights reserved. Source


Lepekha L.N.,Central Tuberculosis Research Institute RAMS | Aleksandrova E.A.,Central Tuberculosis Research Institute RAMS | Evgushchenko G.V.,Central Tuberculosis Research Institute RAMS | Makar'Yants N.N.,Central Tuberculosis Research Institute RAMS | Lovacheva O.V.,Central Tuberculosis Research Institute RAMS
Vestnik Rossiiskoi Akademii Meditsinskikh Nauk | Year: 2012

Application of complex of modem cytologic methods of research bronchoalveolar lavage allowed to allocate most characteristics of development of lymphocytic and macrophagic reaction of bronchial tree in different course of exogenous allergic alveolitis. The most indicative in assessment of origin of exogenous allergic alveolitis development is the characteristics of macrophagic population. In acute course of exogenous allergic alveolitis the considerable number of young activated and non-activated macrophages, increased number of mature phagocytes is observed. Even more significant increase of phagocytic macrophages is observed at dissemination which is primarily is connected with participation of these cells in lymphocytic apoptosis which takes place in high percentage of lymphocytes (up to 49%). Increased number of mature phagocytes is observed at chronic course of exogenous allergic alveolitis that is an important diagnostic pattern of this option of development of exogenous allergic alveolitis in association with the lowest T-helpers/T-supressors index. Source

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