Design, synthesis and biological evaluation of piperazinyl-β-carbolinederivatives as anti-leishmanial agents

Penta Ashok, Subhash Chander, Terry K. Smith, Murugesan Sankaranarayanan

Research output: Contribution to journalArticlepeer-review

14 Citations (Scopus)

Abstract

Molecular hybridization is a ligand based drug design approach is well known recent medicinal chemistry to design anti-parasitic agents. In the present study, we have designed a series of (1-phenyl-9H-pyrido [3,4-b]indol-3-yl) (4-phenylpiperazin-1-yl)methanone derivatives using molecular hybridization approach. Designed analogues were evaluated for cytotoxicity and inhibition activity against Leishmania infantum and Leishmania donovani. Among these reported analogues 7b, 7d, 7e, 7f and 7m displayed potent inhibition of both L. infantum and L. donovani. Compounds 7i and 7k exhibited selective potent inhibition of L. donovani. Especially, compounds 7e and 7k showed most potent anti-leishmanial activity against L. infantum and L. donovani respectively. Anti-leishmanial activity of these compounds is comparable with standard drugs miltefosine and pentamidine. SAR studies revealed that, electron donating group substitution on phenyl ring recommended for potent anti-leishmanial activity.
Original languageEnglish
Pages (from-to)559-566
Number of pages8
JournalEuropean Journal Of Medicinal Chemistry
Volume150
Early online date8 Mar 2018
DOIs
Publication statusPublished - 25 Apr 2018

Keywords

  • Molecular hybridization
  • β-carboline
  • Anti-leishmanial activity

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