Article · Volume 47, Issue 4 · pp. 31–48
Synthesis and preliminary evaluation of a focused chalcone library for anti-inflammatory activity
Ranganathan Balasubramanian1, Hiba Iqbal1, Rachana Vijaya Gopal1, C Baby2
- 1Department of Pharmaceutical Chemistry, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham University, Health Sciences Campus, Kochi-682041, Kerala, India.
- 2Sophisticated Analytical Instrumentation Facility, Indian Institute of Technology, Madras, Chennai-600036, Tamil Nadu, India.
Abstract
A series of monosubstituted chalcones with potential anti-inflammatory activity have been rationally designed leading to a focused library of ligands 4a-j with ring-A substitution. Subsequent to drug-likeness and druggability assessments, the library members were synthesized in optimal yields and their structures were confirmed by IR, 1H NMR, 13C NMR and mass spectral analysis. Screening for anti-inflammatory activity revealed that most of the compounds were quite effective in containing inflammation with compound 4b being the most promising derivative.
Keywords: Chalcones; structure-activity relationship; drug-likeness; anti-inflammatory activity
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