Synthesis and antituberculosis activity of novel unfolded and macrocyclic derivatives of ent-kaurane steviol |
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| Authors: | Ravil N Khaybullin Irina Yu Strobykina Alexey B Dobrynin Aidar T Gubaydullin Regina V Chestnova Vasiliy M Babaev Vladimir E Kataev |
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| Institution: | 1. A.E. Arbuzov Institute of Organic and Physical Chemistry, Kazan Scientific Center, Russian Academy of Sciences, Arbuzov str., 8, Kazan 420088, Russia;2. T.B. Prophylactic Clinical Centre of the Republic of Tatarstan, Ministry of Health of the Republic of Tatarstan, P.Lumuba str., 20, Kazan 420045, Russia |
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| Abstract: | New derivatives of steviol 1, the aglycone of the glycosides of Stevia rebaudiana, including a novel class of semisynthetic diterpenoids, namely macrocyclic ent-kauranes were synthesized. These compounds possess antituberculosis activity inhibiting the in vitro growth of Mycobacterium Tuberculosis (H37RV strain) with MIC 5–20 μg/ml that is close to MIC 1 μg/ml demonstrated by antituberculosis drug isoniazid in control experiment. For the first time it was found that the change of ent-kaurane geometry (as in steviol 1) of tetracyclic diterpenoid skeleton to ent-beyerane one (as in isosteviol 2) influences on antituberculosis activity. |
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