3-Benzylidene-4-chromanones: A novel cluster of anti-tubercular agents

Umashankar Das, Tamas Lorand, Stephen G. Dimmock, Pal Perjesi, Jonathan R. Dimmock

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

In a quest for developing novel anti-tubercular agents, a series of 3-benzylidene-4-chromanones 1a-l were evaluated for growth inhibition of Mycobacterium tuberculosis H37Rv. Three promising compounds 1d, g, j emerged as the lead compounds with the IC50 and IC90 values of less than 1μg/mL. Evaluation of the potent compounds 1d, g, j and k against Vero monkey kidney cells revealed that these compounds are far more toxic to M. tuberculosis than to Vero cells. Structure-activity relationships demonstrated that 3-benzylidene-4-chromanones are more potent against M. tuberculosis than the related 2-benzylidene cycloalkanones and the meta substituted chromanone derivatives are more active than their ortho-and para-counterparts. Some guidelines for amplifying the project are presented.

Original languageEnglish
Pages (from-to)259-263
Number of pages5
JournalJournal of enzyme inhibition and medicinal chemistry
Volume30
Issue number2
DOIs
Publication statusPublished - Apr 1 2015

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Keywords

  • 4-chromanones
  • Anti-mycobacterial
  • Anti-tubercular
  • Structure-activity relationships
  • Tuberculosis
  • Unsaturated ketones

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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