Article Details

SYNTHESIS, BIOLOGICAL EVALUATION AND DOCKING STUDIES OF NON HEPATOTOXIC 5-SUBSTITUTED THIAZOLIDINE-2, 4-DIONES AS ANTIDIABETIC, ANTI-HYPERLIPIDEMIC, ANTI-OXIDANT AND CYTOTOXIC AGENTS

Shukla Karuna S.a,b, Pandey Shailendrac , Chawla A Poojad*

<sup<a Pharmaceutical Research Laboratory, School of Pharmacy, Babu Banarasi Das University, Lucknow - 226 028, Uttar Pradesh, India

b Department of Pharmacy, Goel Institute of Pharmaceutical Sciences, Lucknow - 226 028, Uttar Pradesh, India

c Department of Pharmacy, Sarojini Naidu Medical College, Agra - 282 003, Uttar Pradesh, India

d Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga - 142 001, Punjab, India

* For correspondence E-mail: pvchawla@gmail.com


ABSTRACT

A series of eleven thiazolidine-2, 4-dione (TZD) derivatives, were synthesized and characterized by FT-IR, 1 H NMR and mass spectral analysis. All the synthesized TZD derivatives were screened for their in vitro and in vivo anti-diabetic and antioxidant, activities and cytotoxicity. In vivo antihyperglycemic effect was assessed by measuring plasma glucose (PG) levels in alloxan-induced type II diabetic rat models. The compound 4h exhibited better blood glucose lowering activity than the standard drug rosiglitazone. The synthesized TZD derivatives were evaluated for hepatotoxicity and pancreatic tissue studies. Antioxidant activity was evaluated by DPPH method and H2 O2 method. Compounds 4a and 4b exhibited potent antioxidant activity. Among the tested compounds for cytotoxicity using MTT assay method, compound 4i exhibited better viability and cytotoxicity activity. Thiazolidinedione derivatives were evaluated for their affinity towards target PPARg, using rosiglitazone as the reference compound molecular docking visualization through FlexX docking program. From selected anti-diabetic targets, the proposed derivatives exhibited better interaction with PPARγ receptor, where rosiglitazone showed docking score of -19.891 kJ/ mol, compound 4h exhibited highest docking score of -31.6068 kJ/mol. The study showed that all the studied compounds were showing higher docking score when compared to control drug rosiglitazone and it could be a remarkable starting point to evaluate structure activity relationships to develop new lead molecules with potential anti-diabetic activities.

Year 2020 | Volume No. 57 | Issue No.9 | Page No. 19-37
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