Synthesis and antituberculosis activity of novel unfolded and macrocyclic derivatives of ent-kaurane steviol.
Bioorg Med Chem Lett
; 22(22): 6909-13, 2012 Nov 15.
Article
en En
| MEDLINE
| ID: mdl-23046964
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 (H37R(V) 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.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Diterpenos de Tipo Kaurano
/
Compuestos Macrocíclicos
/
Antituberculosos
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2012
Tipo del documento:
Article
País de afiliación:
Rusia