Library of diversely substituted 2-(quinolin-4-yl)imidazolines delivers novel non-cytotoxic antitubercular leads

Mikhail Krasavin, Prashant Mujumdar, Vladislav Parchinsky, Tatiana Vinogradova, Olga Manicheva, Marine Dogonadze

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

Abstract

A novel library based on quinolin-4-ylimidazoline core was designed to incorporate a general quinoline antimicrobial pharmacophore. A synthesis of the well-characterized library of 36 compounds was achieved using the Pd-catalyzed Buchwald–Hartwig-type imidazoline arylation chemistry developed earlier. Compounds were tested for biological activity and were found to possess no antimalarial activity. However, the library delivered two promising antitubercular leads, which are non-cytotoxic and can be further optimized with respect to antimycobacterial potency.

Original languageEnglish
Pages (from-to)1146-1155
Number of pages10
JournalJournal of Enzyme Inhibition and Medicinal Chemistry
Volume31
Issue number6
DOIs
Publication statusPublished - 1 Nov 2016
Externally publishedYes

Keywords

  • 2-imidazoline
  • Antimalarial
  • antitubercular
  • Buchwald–Hartwig
  • microwave chemistry
  • non-cytotoxic
  • quinoline

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