Design, synthesis, anti-mycobacterial and cytotoxic evaluation of C-4 functionalized 1,8-naphthalimide-heterocyclic hydrazide conjugates

Chem Biol Drug Des. 2019 Jul;94(1):1300-1305. doi: 10.1111/cbdd.13503. Epub 2019 Mar 7.

Abstract

This manuscript discloses the design and synthesis of a series of C-4 functionalized 1,8-naphthalimide-heterocyclic hydrazide conjugates along with their anti-mycobacterial and cytotoxic evaluation. The present work assumes significance as it describes the first report on the amalgamation of C-4 substituted naphthalimides with various heterocyclic hydrazides. However, contrary to the rationale behind the synthesis of the conjugates, none of them inhibited the growth of Mycobacterium tuberculosis at the tested concentrations though these were non-cytotoxic towards the Vero kidney epithelial cell line.

Keywords: anti-mycobacterial; cytotoxicity; heterocyclic hydrazides; isoniazid; naphthalimides.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antitubercular Agents / chemical synthesis*
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology
  • Cell Survival / drug effects
  • Chlorocebus aethiops
  • Drug Design*
  • Hydrazines / chemistry*
  • Isoniazid / chemistry
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects
  • Naphthalimides / chemistry*
  • Vero Cells

Substances

  • Antitubercular Agents
  • Hydrazines
  • Naphthalimides
  • Isoniazid