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Probing 2-acetylbenzofuran hydrazones and their metal complexes as α-glucosidase inhibitors.

Abstract：

:Inhibition of α-glucosidase is one of the important approaches in designing antidiabetic drugs for its role in decrease of the carbohydrates digestion to avoid post-prandial increase in blood sugar levels in diabetic patients. In the present study we designed a novel series of 2-acetylbenzofuran hydrazones (L1-L7) and their metal (II) complexes Cu (II), Co (II), Zn (II) and Mn (II) (8-29) and screened for inhibitory activity against the yeast α-glucosidase. The synthesis of hydrazones incorporated the use of I2 as a catalyst which resulted in excellent yield of 94%. The ligand L3, showed good activity (IC50 = 47.51 ± 0.86 µM) while its metal complex (10) showed potent activity (IC50 = 1.15 ± 0.001 µM) compared to reference acarbose IC50 = 378.25 ± 0.12 µM. Similarly, the Cu (II) complexes with ligands L5 and L6 showed excellent α-glucosidase inhibition (IC50 = 0.15 ± 0.003 12 and 0.21 ± 0.002 µM for 13, respectively) whereas, the metal complexes of Co (II), Mn (II), and Zn (II) showed moderate to poor inhibitory activities against α-glucosidase. The The findings are supported by the ligands and enzyme interactions through molecular docking studies. In conclusion, it is indicated that metal complexes of 2-acetylbenzofuran hydrazones have good potential for research leading to antidiabetic therapies.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Khan S,Tariq M,Ashraf M,Abdullah S,Al-Rashida M,Khalid M,Taslimi P,Fatima M,Zafar R,Shafiq Z

doi

10.1016/j.bioorg.2020.104082

subject

Has Abstract

pub_date

2020-09-01 00:00:00

pages

104082

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(20)31379-1

journal_volume

102

pub_type

杂志文章

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