Affiliation:
1. Department of Chemistry, Faculty of Science, Albaha University, Albaha, Saudi Arabia
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.
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,Pharmaceutical Science,Molecular Medicine
Cited by
4 articles.
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