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INTERNATIONAL JOURNAL OF PHARMACEUTICAL RESEARCH

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Published by : Advanced Scientific Research
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0975-2366
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IJPR 9[3] July - September 2017 Special Issue

July - September 9[3] 2017

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

Author: MANAL F.ALKHAQANI, ALI FATTAH NASER, FARKED WAHOODI SALMAN, AHMED JASIM TWAYEJ, EHAB K. OBAID, ALI JABBAR RADHI
Abstract: A series of new 1,2,3-triazole compounds have been synthesized and tested for their in vitro a-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 a-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 using13CNMR,1HNMR and FTIR.
Keyword: Dapsone, 1,2,3-triazoles, a-glucosidase enzyme, inhibitors.
DOI: https://doi.org/10.31838/ijpr/2020.12.03.358
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