Abstract
The in vivo and in vitro effects of 4,5-diphenylimidazole-2-thione (1), 4,5-Diphenyl-1,2,4-triazole-3-thiol (2) and 5-(2-Hydroxyphenyl)-4-phenyl-1,2,4-triazole-3-thiol (3) on α-glucosidase and α-amylase were investigated. The in vivo inhibition has been found to be dose-dependent and to occur at a value less than LD50. The in vitro treatment of the enzymes by 4,5-diphenylimidazole-2-thione exhibited a reversible inhibition of the non-competitive type with Ki value of 3.5 and 6.5×10−5M for α-glucosidase and α-amylase, respectively. 4,5-Diphenyl-1,2,4-triazole-3-thione showed a reversible inhibition of the competitive and non-competitive types, with Ki value of 10−5M magnitude, for α-glucosidase and α-amylase. On the other hand, 5-(o-hydroxyphenyl)-4-phenyl-1,2,4-triazole-3-thione did not display an inhibitory effect towards α-amylase but showed a potent inhibition of the competitive type for hepatic α-glucosidase with 10−5M magnitude of Ki value.
The in vivo and in vitro inhibitions of α-glucosidase and α-amylase were investigated by diaryl derivatives of imidazole-thione and 1,2,4-triazole-thiol. The in vivo inhibition has been found to be dose-dependent and the in vitro inhibition exhibited a Ki value with 10−5M magnitude. [Display omitted]
► The effect of three compounds of diaryl imidazole and triazole derivatives on α-glucosidase and α-amylase have been examined. ► α-Glucosidase and α-amylase are in vivo inhibited by the three compounds. ► α-Glucosidase is non-competitively or competitively inhibited by the three compounds by in vitro treatment. ► α-Amylase is non-competitively inhibited by only two compounds by in vitro treatment.