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Review
. 2022 Sep 30;15(10):1219.
doi: 10.3390/ph15101219.

A Review of the Biological Activity of Amidrazone Derivatives

Renata Paprocka  1 , Małgorzata Wiese-Szadkowska  2 , Tomasz Kosmalski  1 , Daria Frisch  1 , Magdalena Ratajczak  1 , Bożena Modzelewska-Banachiewicz  1 , Renata Studzińska  1
Affiliations
Review

A Review of the Biological Activity of Amidrazone Derivatives

Renata Paprocka et al. Pharmaceuticals (Basel). .

Abstract

Amidrazones are widely used in chemical synthesis, industry and agriculture. We compiled some of the most important findings on the biological activities of amidrazones described in the years 2010-2022. The data were obtained using the ScienceDirect, Reaxys and Google Scholar search engines with keywords (amidrazone, carbohydrazonamide, carboximidohydrazide, aminoguanidine) and structure strategies. Compounds with significant biological activities were included in the review. The described structures derived from amidrazones include: amidrazone derivatives; aminoguanidine derivatives; complexes obtained using amidrazones as ligands; and some cyclic compounds obtained from amidrazones and/or containing an amidrazone moiety in their structures. This review includes chapters based on compound activities, including: tuberculostatic, antibacterial, antifungal, antiparasitic, antiviral, anti-inflammatory, cytoprotective, and antitumor compounds, as well as furin and acetylocholinesterase inhibitors. Detailed information on the compounds tested in vivo, along the mechanisms of action and toxicity of the selected amidrazone derivatives, are described. We describe examples of compounds that have a chance of becoming drugs due to promising preclinical or clinical research, as well as old drugs with new therapeutic targets (repositioning) which have the potential to be used in the treatment of other diseases. The described examples prove that amidrazone derivatives are a potential source of new therapeutic substances and deserve further research.

Keywords: amidrazone; aminoguanidine; anti-inflammatory; antibacterial; antifungal; antiparasitic; antitumor.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
(a) The general structure of amidrazones, showing the numbering of the nitrogen atoms and the possible phenomenon of tautomerism. (b) The structure of aminoguanidine.
Figure 2
Figure 2
The structures of tuberculostatic compounds 1–8.
Figure 3
Figure 3
The structures of antibacterial compounds 9–32.
Figure 4
Figure 4
The structures of antifungal compounds 33–43.
Figure 5
Figure 5
The structures of antiparasitic compounds 44–51.
Figure 6
Figure 6
The structures of antiviral compounds 52–53.
Figure 7
Figure 7
The structures of anti-inflammatory compounds 54–65.
Figure 8
Figure 8
The structures of cytoprotective compounds 46–48 and 66.
Figure 9
Figure 9
The structures of antitumor compounds 67–91.
Figure 10
Figure 10
The structures of furin inhibitors 92–93.
Figure 11
Figure 11
The structure of compound 94–96.
See this image and copyright information in PMC

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