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Nat Prod Commun ; 11(1): 33-5, 2016 Jan.
Article in English | MEDLINE | ID: mdl-26996014

ABSTRACT

A variety of new and earlier synthesized lupane, oleanane, ursane and dammarane triterpenoids have been investigated for their inhibitory activity against α-glucosidase. 2,3-Indole-21 ß-acetyl-20ß,28-epoxy-18α,19ßH-ursane and 3-oxo-3A-homo-3a-aza-20(S)-hydroxydammar-24(25)-ene were synthesized for the first time. The compounds 3, 4, 8-11 and 14 demonstrated strong in vitro inhibitory activity towards α-glucosidase with IC50 values of 37.5-115.1 µM. 3-Deoxy-3a-homo-3a-aza-28-cinnamoyloxy-20(29)-lupene, with an IC50 of 6.67 µM was 60-fold more active than the market drug acarbose.


Subject(s)
Glycoside Hydrolase Inhibitors/pharmacology , Triterpenes/pharmacology , Glycoside Hydrolase Inhibitors/chemistry , Inhibitory Concentration 50 , Molecular Structure , Oleanolic Acid/analogs & derivatives , Oleanolic Acid/chemistry , Oleanolic Acid/pharmacology , Triterpenes/chemical synthesis , Triterpenes/chemistry , alpha-Glucosidases , Dammaranes
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