Synthesis, characterization, lipoxygenase inhibitory activity and in silico molecular docking of biaryl bis(benzenesulfonamide) and indol-3-yl-hydrazide derivatives

  • Sadaf Mutahir
  • , Muhammad Yar*
  • , Muhammad Asim Khan
  • , Nisar Ullah
  • , Sohail Anjum Shahzad
  • , Islam Ullah Khan
  • , Rana Atif Mehmood
  • , Muhammad Ashraf
  • , Rumana Nasar
  • , Eleni Pontiki
  • *Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

6 Scopus citations

Abstract

Abstract In this paper, we have screened a library of two different series of compounds to identify potent lipoxygenase (LOX) inhibitors. A number of new biphenyl bis(benzenesulfonamides) 2-3, indol-3-yl-benzenesulfonyl and acetohydrazides 4-5 and indol-3-yl-hydrazinecarboxylate 6 were synthesized and evaluated in vitro for LOX inhibitory activity. Compounds biphenyl bis(benzenesulfonamide) 2a and indol-3-yl-benzenesulfonylhydrazide 4e presented the best anti-LOX activity within these series with IC50 values 96.31 ± 0.18 and 81.21 ± 2.14 μM, respectively. The results were confirmed with docking studies.

Original languageEnglish
Article number573
Pages (from-to)1123-1130
Number of pages8
JournalJournal of the Iranian Chemical Society
Volume12
Issue number6
DOIs
StatePublished - 1 Jun 2015

Bibliographical note

Publisher Copyright:
© Iranian Chemical Society 2014.

Keywords

  • Arachidonic acid
  • Baicalein
  • Indole derivatives
  • LOX inhibitors
  • Protein 1RRH

ASJC Scopus subject areas

  • General Chemistry

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