ReviewPost screenThe 1,2,3-triazole ring as a bioisostere in medicinal chemistry

- Triazoles mimic different functional groups, resulting optimal bioisosteres for the synthesis of new active molecules.
- Triazoles present a marked stability under hydrolytic, oxidative and reductive conditions.
- New highly regioselective synthetic methodologies for triazoles synthesis have been recently developed.
- Among the plethora of the selected examples of bioisosterism, the amide bond replacement is clearly a predominant approach.

1,2,3-Triazole is a well-known scaffold that has a widespread occurrence in different compounds characterized by several bioactivities, such as antimicrobial, antiviral, and antitumor effects. Moreover, the structural features of 1,2,3-triazole enable it to mimic different functional groups, justifying its wide use as a bioisostere for the synthesis of new active molecules. Here, we provide an overview of the 1,2,3-triazole ring as a bioisostere for the design of drug analogs, highlighting relevant recent examples.