Affiliation:
1. School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, 144402, Punjab, India
2. I.K. Gujral Punjab Technical University, Jalandhar, Punjab, India
3. Department of Pharmaceutical Chemistry, Shivalik College of Pharmacy, Nangal, Dist. Rupnagar, 140126, Punjab, India
Abstract
Background:
Indole and its derivatives have a wide range of pharmacological effects,
including analgesic, antimicrobial, antidepressant, anti-diabetic, anti-convulsant, anti-helminthic,
and anti-inflammatory properties. They are crucial structural components of many of today's powerful
antioxidant medications.
Objective:
Using the Schotten–Baumann reaction, the indole ring was linked to other key heterocyclic
moieties such as morpholine, imidazole, piperidine, and piperazine at the active 3rd position
and then tested for antioxidant activity.
Methods:
Synthesis of derivatives was accomplished under appropriate conditions and characterized
by IR, NMR (1H and 13C), and mass spectrum. Using the Swiss ADME online application,
ADME properties were also determined. The in vitro antioxidant activity was measured using
DPPH and Reducing power method.
Results:
In the DPPH assay, compounds 5a (IC50=1.01±0.22 μg/mL), 5k (IC50=1.21±0.07μg/mL),
whereas compounds 5a (EC50=23±1.00 μg/mL), 5h (EC50=26±2.42 μg/mL) in the reducing power assay
were most potent as compared with standard Ascorbic acid. Compounds 5a, 5h, and 5k demonstrated
maximal potency equivalent to standard. Lipinski's rule was followed in ADME outcomes.
Conclusion:
The synthesis and evaluation of indole derivatives to investigate their antioxidant action
has received a lot of attention. These discoveries could lead to more effective antioxidant candidates
being designed and developed.
Publisher
Bentham Science Publishers Ltd.
Subject
Organic Chemistry,Computer Science Applications,Drug Discovery,General Medicine
Cited by
3 articles.
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