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Synthesis, In Silico Pharmacokinetics, and Biological Evaluation of Some New Thiazolidinedione as PPAR-γ Agonists and Antibacterial Agents

[ Vol. 18 , Issue. 10 ]

Author(s):

Zohor Mohammad Mahdi Alzhrani, Mohammad Mahboob Alam and Syed Nazreen*   Pages 998 - 1008 ( 11 )

Abstract:


Background: The frequent use of antimicrobial agents to treat infections in diabetic patients make them more drug resistant than non-diabetic patients, which accounts for a higher mortality rate of diabetic patients. Therefore, it is a necessity today to synthesize new drugs with dual modes of action as antidiabetic and antibacterial agents. In the present work, new derivatives containing thiazolidinedione and 1,3,4-oxadiaozle have been synthesized and screened for PPAR-γ and antibacterial activities.

Methods: Compounds 5-12 have been synthesized from 2-methoxy benzaldehyde and thiazolidinedione and characterized using different spectroscopic techniques such as IR, NMR, and mass spectrometry. These compounds were tested for in vitro PPAR-γ transactivation, PPAR-γ gene expression, and antibacterial activities. Finally, molecular docking was carried out to see the binding interactions of molecules with the target protein.

Results: All the compounds follow the Lipinski rule suggesting the synthesized derivatives have good drug-likeness properties. Compounds 11 and 12 exhibited promising PPAR-γ transactivation with 73.69% and 76.50%, respectively, as well as showed significant antibacterial activity with comparable MIC of 3.12 μg/disc to standard drug amoxicillin. The docking result was found to be consistent with the in vitro PPAR-γ transactivation results.

Conclusion: Compounds 11 and 12 can be further investigated as lead molecules for the development of new and effective antidiabetic and antibacterial agents.

Keywords:

Thiazolidinedione, pharmacokinetics, PPAR-γ, antibacterial, molecular docking, diabetic patients.

Affiliation:

Department of Chemistry, Faculty of Science, Albaha University, Albaha, Department of Chemistry, Faculty of Science, Albaha University, Albaha, Department of Chemistry, Faculty of Science, Albaha University, Albaha



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