N-Acylhydrazones as drugs

Bioorg Med Chem Lett. 2018 Sep 15;28(17):2797-2806. doi: 10.1016/j.bmcl.2018.07.015. Epub 2018 Jul 9.


Over the last two decades, N-acylhydrazone (NAH) has been proven to be a very versatile and promising motif in drug design and medicinal chemistry. Herein, we discuss the current and future challenges in the emergence of bioactive NAH-based scaffolds and to developing strategies to overcome the failures in drug discovery. The NAH-related approved drugs nitrofurazone, nitrofurantoin, carbazochrome, testosterone 17-enanthate 3-benzilic acid hydrazine, nifuroxazide, dantrolene, and azumolene are already used as therapeutics in various countries. PAC-1 is an NAH-based therapeutic agent that entered clinical trials in 2015. Another NAH-derived scaffold, LASSBio-294, is in preclinical trials. This review highlights the detailed comprehensive assessment and therapeutic landscape of bioactive NAH motif scaffolds in preclinical and clinical studies published to date and their promise and associated challenges in current and future drug discovery of NAH-based drugs that will progress to clinical use.

Keywords: Clinical trials; Drug discovery; Drugs; N-Acylhydrazone; Preclinical; Therapeutics.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / therapeutic use*
  • Drug Discovery
  • Humans
  • Hydrazones / chemistry
  • Hydrazones / therapeutic use*
  • Molecular Structure
  • Neoplasms / drug therapy*


  • Antineoplastic Agents
  • Hydrazones