Lipid Lowering Oxopropanylindole Hydrazone Derivatives with Anti-oxidant and Anti-hyperglycemic Activity

被引:3
作者
Varshney, Kanika [1 ]
Gupta, Amit K. [2 ]
Sonkar, Ravi [3 ]
Varshney, Salil [4 ]
Mishra, Akanksha [3 ]
Bhatia, Geetika [3 ]
Gaikwad, Anil [4 ]
Srivastava, Arvind Kumar [3 ]
Saxena, Mridula [5 ]
Jain, Sudha [6 ]
Saxena, Anil K. [1 ]
机构
[1] Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226031, Uttar Pradesh, India
[2] Univ Texas Hlth Sci Ctr Houston, McGovern Med Sch, Dept Integrat Biol & Pharmacol, Houston, TX 77030 USA
[3] Cent Drug Res Inst, Biochem Div, Lucknow 226031, Uttar Pradesh, India
[4] Cent Drug Res Inst, Pharmacol Div, Lucknow 226031, Uttar Pradesh, India
[5] Amity Univ, Dept Chem, Lucknow, Uttar Pradesh, India
[6] Lucknow Univ, Dept Chem, Lucknow 226007, Uttar Pradesh, India
关键词
Hydrazone derivatives; Anti-oxidant; Anti-dyslipidemic; Atherosclerosis; Lipid; Anti-hyperglycemic; LOW-DENSITY-LIPOPROTEIN; CORONARY-HEART-DISEASE; ATHEROSCLEROSIS; IDENTIFICATION; CHOLESTEROL; LIPASE; INHIBITORS; PROTEIN; HDL;
D O I
10.2174/1568026619666181220112903
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of substituted oxopropanylindole hydrazone derivatives was synthesized and evaluated for anti-oxidant and anti-dyslipidemic activity. Of the 12 tested, 3 compounds (6c, 7b and 7d) showed good anti-oxidant activity, compound 6c attenuated LDL oxidation by 32%. The compounds 6c and 7d also showed good anti-dyslipidemic activity by reducing serum levels of total cholesterol (TC), phospholipids (PL) and triglycerides (TG). These two compounds were further evaluated for anti-adipogenic and anti-hyperglycemic activity, where 6c showed 44% reduction in lipid accumulation and 20.5% and 24.3% reduction in blood glucose at 5h and 24h respectively, as compared to standard drug metformin. Thus, compounds 6c and 7d with balanced anti-oxidant and anti-dyslipidimic activities may be excellent candidates for lead optimization and drug development for the treatment of metabolic disorders.
引用
收藏
页码:2256 / 2265
页数:10
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