Synthesis and Biological Evaluation of Some New Rhodanine Analogues as Aldose Reductase Inhibitors (ARIs)

  • Neelam Khan Research Scholar, Bhagwant University, Ajmer (Raj.), India
  • Girendra Gautam Bhagwant University, Ajmer (Raj.), India
  • Arun K. Gupta Chamelidevi Institute of Pharmacy, Indore (M.P.), India

Abstract

Diabetes mellitus is a metabolic disorder characterized by hyperglycemia resulting long-term secondary complication. Aldose reductase, the rate-limiting enzyme of the polyol pathway, plays a key role in the treatment of diabetic complications. Appropriately, inhibition of this enzyme is emerging as a major therapeutic strategy for the pathogenesis of secondary complication. In this study, we describe a series of 5 aryl benzylidene -thiazolidine, 4-dione derivatives, F3 synthesized as aldose reductase inhibitors. Besides inhibiting efficiently the target enzyme, F4 and F5 showed additional AR inhibitory as well as hypoglycaemic activity (146.15 and 175.20 mg/dl ) thus emerging as novel dual acting compounds. The bezylidene derivative F3, the most promising of the whole series, showed a well-balanced, consisting of ALR2 inhibitory efficacy (83.00% at 10µg/mL), similarly, F3 have lower blood glucose level in the range of 131.11 mg/dl at 15 mg/kg body weight. This compound show robust in vitro and in vivo efficacy, and could be considered as promising dual target antidiabetic drug candidates.


Keywords: Diabetes mellitus, hyperglycemia, Aldose reductase inhibitors

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Author Biographies

Neelam Khan, Research Scholar, Bhagwant University, Ajmer (Raj.), India

Research Scholar, Bhagwant University, Ajmer (Raj.), India

Girendra Gautam, Bhagwant University, Ajmer (Raj.), India

Bhagwant University, Ajmer (Raj.), India

Arun K. Gupta, Chamelidevi Institute of Pharmacy, Indore (M.P.), India

Chamelidevi Institute of Pharmacy, Indore (M.P.), India

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How to Cite
Khan, N., Gautam, G., & Gupta, A. K. (2019). Synthesis and Biological Evaluation of Some New Rhodanine Analogues as Aldose Reductase Inhibitors (ARIs). Journal of Drug Delivery and Therapeutics, 9(1-s), 161-167. https://doi.org/10.22270/jddt.v9i1-s.2284