Abstract
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 antiadipogenic 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.
Keywords: Hydrazone derivatives, Anti-oxidant, Anti-dyslipidemic, Atherosclerosis, Lipid, Anti-hyperglycemic.
Graphical Abstract
Current Topics in Medicinal Chemistry
Title:Lipid Lowering Oxopropanylindole Hydrazone Derivatives with Antioxidant and Anti-hyperglycemic Activity
Volume: 18 Issue: 26
Author(s): Kanika Varshney, Amit K. Gupta, Ravi Sonkar, Salil Varshney, Akanksha Mishra, Geetika Bhatia, Anil Gaikwad, Arvind Kumar Srivastava, Mridula Saxena, Sudha Jain*Anil K. Saxena*
Affiliation:
- Department of Chemistry, Lucknow University, Lucknow, 226007,India
- Medicinal & Process Chemistry Division, Central Drug Research Institute, Lucknow, 226031,India
Keywords: Hydrazone derivatives, Anti-oxidant, Anti-dyslipidemic, Atherosclerosis, Lipid, Anti-hyperglycemic.
Abstract: 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 antiadipogenic 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.
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Cite this article as:
Varshney Kanika , Gupta K. Amit , Sonkar Ravi , Varshney Salil , Mishra Akanksha, Bhatia Geetika , Gaikwad Anil , Srivastava Kumar Arvind , Saxena Mridula, Jain Sudha*, Saxena K. Anil *, Lipid Lowering Oxopropanylindole Hydrazone Derivatives with Antioxidant and Anti-hyperglycemic Activity, Current Topics in Medicinal Chemistry 2018; 18 (26) . https://dx.doi.org/10.2174/1568026619666181220112903
DOI https://dx.doi.org/10.2174/1568026619666181220112903 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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