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

Author:

Varshney Kanika1,Gupta Amit K.2,Sonkar Ravi3,Varshney Salil4,Mishra Akanksha3,Bhatia Geetika3,Gaikwad Anil4,Srivastava Arvind Kumar3,Saxena Mridula5,Jain Sudha6,Saxena Anil K.1

Affiliation:

1. Medicinal & Process Chemistry Division, Central Drug Research Institute, Lucknow, 226031, India

2. Department of Integrative Biology and Pharmacology, McGovern Medical School, University of Texas Health Science Center at Houston, Houston, TX 77030, United States

3. Biochemistry Division, Central Drug Research Institute, Lucknow, 226031, India

4. Pharmacology Division, Central Drug Research Institute, Lucknow, 226031, India

5. Department of Chemistry, Amity University, Lucknow, India

6. Department of Chemistry, Lucknow University, Lucknow, 226007, India

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.

Publisher

Bentham Science Publishers Ltd.

Subject

Drug Discovery,General Medicine

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