3 years ago

Synthesis and evaluation of 2,3-indolotriterpenoids as new α-glucosidase inhibitors

Oxana B. Kazakova, Do Quoc Viet, Nguyen Thi Thu Ha, Anastasiya V. Petrova, Elmira F. Khusnutdinova, Irina E. Smirnova

Abstract

A series of ring-A fused heterocycles of lupane, oleanane, ursane and dammarane triterpenoids were synthesized and evaluated for their inhibitory activity against α-glucosidase. An influence of the different types of triterpenoids with indole and pyrazine cycles on the activity was revealed. Among them, 2,3-indolo-lup-20(29)-en-28-oic acid with an IC50 of 1.8 µM was the most active compound being 221-fold more active than the market drug acarbose. In the most cases, the replacement of the indole by the pyrazine fragment provided the decreasing of activity (except dammarane type pyrazine derivative).

Graphical Abstract

Publisher URL: https://link.springer.com/article/10.1007/s00044-017-1972-0

DOI: 10.1007/s00044-017-1972-0

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