Synthesis of new dapsone derivatives linked 1,2,3-triazole ring as α-glucosidase inhibitors.

Autor: ALKHAQANI, MANAL F., NASER, ALI FATTAH, SALMAN, FARKED WAHOODI, TWAYEJ, AHMED JASIM, OBAID, EHAB K., RADHI, ALI JABBAR
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Zdroj: International Journal of Pharmaceutical Research (09752366); Jul-Sep2020, Vol. 12 Issue 3, p2553-2556, 4p
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]
Databáze: Complementary Index