Research on Guanidine-Based Drugs: Synthesis, Antiparasitic, Antifungal, Antiviral, and Anticancer Activities

Dear Colleagues,

Guanidine-based compounds have long attracted interest due to their remarkable chemical versatility and broad spectrum of biological activities. Historically, guanidine derivatives were first explored for their antimicrobial and antiparasitic effects. Over the decades, their therapeutic potential has expanded significantly. These molecules exhibit strong interactions with biological targets due to their unique basicity and hydrogen-bonding capabilities, making them promising scaffolds in drug discovery. Recent advancements in synthetic methodologies, such as metal-catalyzed reactions, multicomponent reactions, and green chemistry approaches, have further facilitated the design and functionalization of guanidine frameworks. These innovations have enabled the development of structurally diverse and biologically potent analogs. In addition to their well-known antiparasitic applications, the results of recent studies have highlighted the antifungal, antiviral, and anticancer potential of guanidine-based drugs. These findings open new avenues for therapeutic intervention, particularly in the context of neglected tropical diseases and emerging infectious agents. Innovations in medicinal chemistry and structure–activity relationship (SAR) analyses have enabled a deeper understanding of their mechanisms of action. This progress is paving the way for more targeted and effective treatment strategies.

The aim of the following Special Issue is to provide a comprehensive overview of recent advances in the synthesis and pharmacological exploration of guanidine derivatives, with particular emphasis on innovative approaches and emerging therapeutic perspectives. The focus is on the development of safer and more effective drug candidates capable of addressing both persistent and emerging global health challenges.

Dr. Eduardo René Pérez González
Dr. Eduardo Henrique Zampieri
Dr. Francisco Jaime Bezerra Mendonça-Junior
Dr. Eduardo Maffud Cilli
Dr. Ana Marisa Fusco Almeida
Guest Editors

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