Synthesis and Biological Activity of Hydrazones and Derivatives: A Review

Abstract

Hydrazones and their derivatives are very important compounds in medicinal chemistry due to their reported biological activity for the treatment of several diseases, like Alzheimer’s, cancer, inflammation, and leishmaniasis. However, most of the investigations on hydrazones available in literature today are directed to the synthesis of these molecules with little discussion available on their biological activities. With the purpose of bringing lights into this issue, we performed a revision of the literature and wrote this review based on some of the most current research reports of hydrazones and derivatives, making it clear that the synthesis of these molecules can lead to new drug prototypes. Our goal is to encourage more studies focused on the synthesis and evaluation of new hydrazones, as a contribution to the development of potential new drugs for the treatment of various diseases.

Synthesis of Novel N-Acylhydrazones and Their C-N/N-N Bond Conformational Characterization by NMR Spectroscopy

“…This moiety is a putative bioisostere of amide backbone [9]. Its achiral nature and higher chemical stability than peptide bond have urged the medicinal chemists to consider this privileged scaffold for structural design of new drug candidates [10][11][12][13][14][15][16]. Due to the presence of H-bonding sites and viability of adopting multiple conformational orientations, N-acylhydrazones have a promising prospective to interact with various bioreceptors.…”

Novel N-Substituted Amino Acid Hydrazone-Isatin Derivatives: Synthesis, Antioxidant Activity, and Anticancer Activity in 2D and 3D Models In Vitro

“…Hydrazone derivatives, whose biological activity is associated with the presence of the active azomethine pharmacophore, constitute another significant class of biologically active compounds in medicinal and pharmaceutical chemistry [25]. These compounds, in combination with various heterocyclic scaffolds, produce diverse biological results, including antioxidant and anticancer activities [26][27][28].…”

Thiosemicarbazone Complexes of Transition Metals as Catalysts for Cross-Coupling Reactions

“…One of the primary motivations for research into these complexes has been the various areas in which they have been proposed for application. For example, apart from their activity as catalysts, which will be covered in more detail in this review, many thiosemicarbazone metal complexes have been widely studied as potential treatments for various types of cancer, for viral, bacterial, or fungal infections, and for neurodegenerative diseases, or for malaria [17][18][19][20][21][22][23][24][25][26]. Thiosemicarbazone metal complexes have also found potential application in medical imaging [27,28], while thiosemicarbazones themselves show promise as metal ion sensors and for the scavenging of metals due to their selective and specific coordination properties [28][29][30][31][32][33][34].…”