Tuberculostatic Activity of 2-Amino-6-Chloropurine Derivatives
- Authors: Kravchenko M.A.1, Skornyakov S.N.1, Bekker O.B.2, Maslov D.A.2, Danilenko V.N.2, Charushin V.N.3, Krasnov V.P.3, Vigorov A.Y.3, Gruzdev D.A.3, Levit G.L.3
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Affiliations:
- Urals Science Research Institute of Phthysiopulmonology
- N. I. Vavilov Institute of General Genetics, Russian Academy of Sciences
- I. Ya. Postovskii Institute of Organic Synthesis, Urals Branch, Russian Academy of Sciences
- Issue: Vol 51, No 9 (2017)
- Pages: 769-772
- Section: Article
- URL: https://journals.rcsi.science/0091-150X/article/view/244795
- DOI: https://doi.org/10.1007/s11094-017-1690-4
- ID: 244795
Cite item
Abstract
Studies of the antimycobacterial activity of 2-amino-6-chloropurine and its N-acyl derivatives against laboratory (Mycobacterium tuberculosis H37Rv, M. avium, M. terrae) and clinical Mycobacterium tuberculosis strains (MDR-TB) identified compounds with high tuberculostatic activity (MIC from 0.35 – 1.5 μg/ml). The cytotoxic activities of the compounds with antimycobacterial activity against human embryo fibroblasts were studied in the MTT test, which showed that the study compounds were essentially nontoxic (IC50 > 50 μM). Further chemical modification may yield compounds with potential for creating drugs for the treatment of tuberculosis. With the aim of identifying the possible mechanism of the tuberculostatic activity, the ability of the study compounds to inhibit mycobacterial serine-threonine protein kinases (STPK) was assessed. The tuberculostatic activity of 2-amino-6-chloropurine derivatives was not linked with their inhibition of STPK.
Keywords
About the authors
M. A. Kravchenko
Urals Science Research Institute of Phthysiopulmonology
Email: ca@ios.uran.ru
Russian Federation, 50 XXII Parts”ezd Street, Ekaterinburg, 620039
S. N. Skornyakov
Urals Science Research Institute of Phthysiopulmonology
Email: ca@ios.uran.ru
Russian Federation, 50 XXII Parts”ezd Street, Ekaterinburg, 620039
O. B. Bekker
N. I. Vavilov Institute of General Genetics, Russian Academy of Sciences
Email: ca@ios.uran.ru
Russian Federation, 3 Gubkin Street, GSP-1, Moscow, 119991
D. A. Maslov
N. I. Vavilov Institute of General Genetics, Russian Academy of Sciences
Email: ca@ios.uran.ru
Russian Federation, 3 Gubkin Street, GSP-1, Moscow, 119991
V. N. Danilenko
N. I. Vavilov Institute of General Genetics, Russian Academy of Sciences
Email: ca@ios.uran.ru
Russian Federation, 3 Gubkin Street, GSP-1, Moscow, 119991
V. N. Charushin
I. Ya. Postovskii Institute of Organic Synthesis, Urals Branch, Russian Academy of Sciences
Email: ca@ios.uran.ru
Russian Federation, S. Kovalevskaya Street, 20/22 Akademicheskaya, Ekaterinburg, 620990
V. P. Krasnov
I. Ya. Postovskii Institute of Organic Synthesis, Urals Branch, Russian Academy of Sciences
Author for correspondence.
Email: ca@ios.uran.ru
Russian Federation, S. Kovalevskaya Street, 20/22 Akademicheskaya, Ekaterinburg, 620990
A. Yu. Vigorov
I. Ya. Postovskii Institute of Organic Synthesis, Urals Branch, Russian Academy of Sciences
Email: ca@ios.uran.ru
Russian Federation, S. Kovalevskaya Street, 20/22 Akademicheskaya, Ekaterinburg, 620990
D. A. Gruzdev
I. Ya. Postovskii Institute of Organic Synthesis, Urals Branch, Russian Academy of Sciences
Email: ca@ios.uran.ru
Russian Federation, S. Kovalevskaya Street, 20/22 Akademicheskaya, Ekaterinburg, 620990
G. L. Levit
I. Ya. Postovskii Institute of Organic Synthesis, Urals Branch, Russian Academy of Sciences
Email: ca@ios.uran.ru
Russian Federation, S. Kovalevskaya Street, 20/22 Akademicheskaya, Ekaterinburg, 620990