Conjugates of the diterpenoid isosteviol (16-oxo-ent-beyeran-19-oic acid) and the drug dimephosphon (1,1dimethyl-3-oxobutylphosphonic acid dimethyl ester) were synthesized. They inhibited completely growth of M. tuberculosis (H37Rv, in vitro) with MIC values of 5–10 μg/mL (MIC value of the antituberculosis drug isoniazid in a control was 0.5 μg/mL).
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Acknowledgment
The work was supported financially by the RAS Presidium Program No. 8 “Development of Organic Synthesis Methods and Creation of Compounds with Valuable Applied Properties”; the RAS OKhNM program No. 6 “Chemistry and Physicochemistry of Supramolecular Systems and Atomic Clusters”; and the RFBR (Grant No. 10-03-00499-a).
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Translated from Khimiya Prirodnykh Soedinenii, No. 5, September–October, 2012, pp. 710–713.
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Garifullin, B.F., Chestnova, R.V., Mironov, V.F. et al. Synthesis and antituberculosis activity of conjugates of the diterpenoid isosteviol and the drug dimephosphon. Chem Nat Compd 48, 794–798 (2012). https://doi.org/10.1007/s10600-012-0385-z
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DOI: https://doi.org/10.1007/s10600-012-0385-z