Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates

Siva S. Panda, Adel S. Girgis, Sean J. Thomas, Jason E. Capito, Riham F. George, Asmaa Salman, May A. El-Manawaty, Ahmed Samir

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

Abstract

A series of curcumin bis-conjugates 3a-q, 5a-k and 6a-k were synthesized in good yields utilizing an optimized reaction condition. We explored the effect of different amino acids and protecting groups on biological activities of curcumin. The conjugates were screened for anti-inflammatory, analgesic and antimicrobial properties. Some of the conjugates showed promising biological observations with a potency comparable with the standard references. The variations in biological properties concerning different amino acids and protecting groups are interesting observations. Effects of the synthesized conjugates on splenocytes and the production of nitric oxide by lipopolysaccharide-stimulated peritoneal macrophages are correlated with the observed anti-inflammatory properties. We have also established the safety profile of the most active conjugates. Robust 2D-QSAR studies supported and validated biological data.

Original languageEnglish (US)
Article number112293
JournalEuropean Journal of Medicinal Chemistry
Volume196
DOIs
StatePublished - Jun 15 2020

Keywords

  • 2D-QSAR
  • Amino acid
  • Analgesic
  • Anti-inflammatory
  • Antimicrobial
  • Curcumin
  • Prodrug

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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