Design, and facile synthesis of 1,3 diaryl-3-(arylamino)propan-1-one derivatives as the potential alpha-amylase inhibitors and antioxidants

被引：51

作者：

Bashary, Roqia ^{[1
,2
]}

Khatik, Gopal L. ^{[2
]}

机构：

[1] Kabul Univ, Dept Pharmaceut Chem, Kabul, Afghanistan

[2] Lovely Profess Univ, Sch Pharmaceut Sci, Dept Pharmaceut Chem, Phagwara 144411, Punjab, India

来源：

BIOORGANIC CHEMISTRY | 2019年 / 82卷

关键词：

Diabetes; Antidiabetic; Alpha-amylase inhibitor; Aza-Michael addition; Antioxidant; AZA-MICHAEL ADDITION; CONJUGATE ADDITION; REUSABLE CATALYST; AMINES; EFFICIENT; ACID; PROTOCOL; DOCKING; ESTERS;

D O I：

10.1016/j.bioorg.2018.10.010

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Diabetes is the most prevalent metabolic disorder causing a high rate of mortality and morbidity. Recently alpha-amylase is reported to be good drug design target for the treatment of diabetes mellitus. We have designed 116 molecules based on aza-Michael adduct of trans-chalcone as 1,3 diaryl-3-(arylamino)propan-1-ones which were studied by molecular docking and among them best six derivatives were synthesized easily via aza-Michael addition on trans-chalcone using KOH as a catalyst and evaluated for alpha-amylase inhibition along with antioxidant activity. It was observed that all compounds have alpha-amylase inhibitory activity but at different extents. The molecule 3e is the most potent alpha-amylase inhibitor of this series. 3a is the second most potent compound, whereas only one molecule 3d has shown antioxidant activity.

引用

页码：156 / 162

页数：7

共 35 条

[1]

Adeghate Ernest, 2011, Open Med Chem J, V5, P68, DOI 10.2174/1874104501105010068

[2] From carbohydrates to drug-like fragments: Rational development of novel α-amylase inhibitors [J].