TB Research

Design and synthesis of 4-Aminoquinoline-isoindoline-dione-isoniazid triads as potential anti-mycobacterials

Rani A, Johansen MD, Roquet-Banères F, Kremer L, Awolade P, Ebenezer O, Singh P, Sumanjit, et al. (9 authors)

Bioorganic & medicinal chemistry letters · 2020-09

Abstract

A series of 4-aminoquinoline-isoindoline-dione-isoniazid triads were synthesized and assessed for their anti-mycobacterial activities and cytotoxicity. Most of the synthesized compounds exhibited promising activities against the mc 2 6230 strain of M. tuberculosis with MIC in the range of 5.1-11.9 µM and were non-cytotoxic against Vero cells. The conjugates lacking either isoniazid or quinoline core in their structural framework failed to inhibit the growth of M. tuberculosis; thus, further strengthening the proposed design of triads in the present study.

MeSH terms

  • Mycobacterium tuberculosis
  • Isoniazid
  • Indoles
  • Aminoquinolines
  • Antitubercular Agents
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Structure-Activity Relationship
  • Dose-Response Relationship, Drug
  • Drug Design