1,2,3-Triazoles in Drug Discovery: Expanding Horizons in Medicinal Chemistry

1,2,3-Triazoles are privileged five-membered aromatic heterocycles featuring three consecutive nitrogen atoms, and have emerged as versatile scaffolds in medicinal chemistry. The incorporation of the 1,2,3-triazole ring into drug molecules has led to the development of several approved therapeutics, including the antibacterials tazobactam and cefatrizine, the anticancer agents carboxyamidotriazole (CAI) and mubritinib, the anti-HIV compound TSAO, and the anticonvulsant rufinamide.Beyond these examples, 1,2,3-triazole derivatives have demonstrated a wide spectrum of biological activities—such as anti-inflammatory, antidiabetic, antiprotozoal, antifungal, and more—showcasing their broad pharmacological potential. These effects are attributed to the unique physicochemical properties of the 1,2,3-triazole moiety, which acts as a bioisostere for amides and frequently mimics both trans- and cis-amide bonds, depending on its substitution pattern.The prominence of 1,2,3-triazoles is further enhanced by their straightforward and efficient synthesis, particularly through regioselective 1,3-dipolar cycloaddition ('click chemistry') and emerging sustainable methodologies that minimize environmental impact.This Research Topic invites original research articles, reviews, and perspectives focused on the role of 1,2,3-triazoles in drug discovery and development. Areas of interest include, but are not limited to:o Design and synthesis of novel 1,2,3-triazole compoundso Pharmacological evaluation and mechanism-of-action studieso Structure-activity relationships and bioisosteric replacementso Innovative synthetic methodologies, including sustainable and green chemistry approacheso Applications in diverse therapeutic areasWe encourage contributions exploring experimental and computational advances, as well as interdisciplinary research that highlights the multifaceted potential of 1,2,3-triazoles in modern pharmacology and drug development. Please note that submissions lacking experimental validation of in silico findings will not be considered. Topic editors: Daniel Tadeu Gomes Gonzaga, David Rodrigues Da Rocha, Vitor Ferreira Source: https://www.frontiersin.org/research-topics/73704/123-triazoles-in-drug-discovery-expanding-horizons-in-medicinal-chemistry