Design, synthesis and docking studies of new quinoline-3-carbohydrazide derivatives as antitubercular agents

K. D. Thomas, Airody Vasudeva Adhikari, Sandeep Telkar, Imran H. Chowdhury, Riaz Mahmood, Nishith K. Pal, Guru Row, E. Sumesh

Research output: Contribution to journalArticlepeer-review

86 Scopus citations

Abstract

Three new series of 4-hydroxy-8-trifluoromethyl-quinoline derivatives were synthesized through multi step reactions. All the newly synthesized compounds were characterized by spectral and elemental analyses. The structure of 5j was evidenced by X-ray crystallographic study. The newly synthesized title compounds were evaluated for their antimicrobial activities including antimycobacterial activity. Amongst the tested compounds, 5b, 5e, 5h, 5j, 6c and 7c displayed promising antimicrobial activity. The mode of action of these active compounds was carried out by docking of receptor enoyl-ACP reductase with newly synthesized candidate ligands, 5b, 5e, 5h, 5j and 6c.

Original languageEnglish (US)
Pages (from-to)5283-5292
Number of pages10
JournalEuropean journal of medicinal chemistry
Volume46
Issue number11
DOIs
StatePublished - Nov 2011
Externally publishedYes

Keywords

  • Antibacterial
  • Antimycobacterial
  • Docking study
  • Quinoline
  • X-ray crystallography

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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