Synthesis and preliminary evaluation of a focused chalcone library for anti-inflammatory activity

Indian Journal of Pharmaceutical Education and Research

  • Ranganathan Balasubramanian1Department of Pharmaceutical Chemistry, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham University, Health Sciences Campus, Kochi-682041, Kerala, India.
  • Hiba Iqbal1Department of Pharmaceutical Chemistry, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham University, Health Sciences Campus, Kochi-682041, Kerala, India.
  • Rachana Vijaya Gopal1Department of Pharmaceutical Chemistry, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham University, Health Sciences Campus, Kochi-682041, Kerala, India.
  • C Baby2Sophisticated Analytical Instrumentation Facility, Indian Institute of Technology, Madras, Chennai-600036, Tamil Nadu, India.

Volume 47 Issue 4 Pages 31-48

DOI: 10.5530/ijper.47.4.5

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
IJOPP

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