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 compounds
o Pharmacological evaluation and mechanism-of-action studies
o Structure-activity relationships and bioisosteric replacements
o Innovative synthetic methodologies, including sustainable and green chemistry approaches
o Applications in diverse therapeutic areas
We 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.
Article types and fees
This Research Topic accepts the following article types, unless otherwise specified in the Research Topic description:
Brief Research Report
Case Report
Clinical Trial
Data Report
Editorial
FAIR² Data
General Commentary
Hypothesis and Theory
Methods
Articles that are accepted for publication by our external editors following rigorous peer review incur a publishing fee charged to Authors, institutions, or funders.
Article types
This Research Topic accepts the following article types, unless otherwise specified in the Research Topic description:
Brief Research Report
Case Report
Clinical Trial
Data Report
Editorial
FAIR² Data
General Commentary
Hypothesis and Theory
Methods
Mini Review
Opinion
Original Research
Perspective
Review
Systematic Review
Technology and Code
Keywords: 1, 2, 3-Triazoles, Medicinal Chemistry, Click Chemistry, Bioisosteres, Drug Discovery, Pharmacological Evaluation, Green Synthesis
Important note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.
