Betulinic acid derivatives: a new class of α-glucosidase inhibitors and LPS-stimulated nitric oxide production inhibition on mouse macrophage RAW 264.7 cells

Chemical manipulation studies were conducted on betulinic acid (1), twenty-one new rationally designed analogues of 1 with modifications at C-28 were synthesized for their evaluation of inhibitory effects on alpha-glucosidase and LPS-stimulated nitric oxide production in mouse macrophage RAW 264.7 cells. Compound 2 (IC50 = 5.4 mu M) exhibited an almost 1.4-fold increase in alpha-glucosidase inhibitory activity on yeast alpha-glucosidase while analogues 5 (IC50 16.4 mu M) and 11 (IC50 16.6 mu M) exhibited a 2-fold enhanced inhibitory activity on NO-production than betulinic acid. [GRAPHICS] .