Abstrakt: |
A series of new 1,2,3-triazole compounds have been synthesized and tested for their in vitro α-glucosidase inhibitory activity. At first dapsone was converted to 4,4'-sulfonylbis(azidobenzene) through reaction dapsone with sodium nitrate and concentrated hydrochloric acid to form diazonum salt and then with sodium azide. 1,2,3-triazoles were prepared by reaction 4,4'-sulfonylbis(azidobenzene) with some triple bond derivatives such as propargylbromide, propargylchloride, propargylalcohol, 1-nitro-3-(prop-2-ynyloxy)benzene and 1-(prop-2- ynyloxy) naphthalene by using click reaction conditions. All 1,2,3-triazole derivatives were showed α- glucosidase inhibition in which compounds 4, 5 and 7 demonstrated the highest activity with IC50 values ranging from 91.28 to 125.14µM, when compared to the standard drug acarbose IC50= 878.38 µM . Structures of prepared derivatives were identified by using 13CNMR,¹HNMR and FTIR. [ABSTRACT FROM AUTHOR] |