Coumarin, a 2H-chromen-2-one oxa-heterocycle, has been extensively studied due to its occurrence in many biologically active compounds, such as Umbelliferon, the anticoagulants acenocoumarin and Warfarin, and the antibiotic Novobiocin. The ubiquity of coumarin is most likely due to its chemical structure flat, aromatic, and lipophilic with a lactone group that allows for binding to diverse targets through hydrophobic, π–π stacking, hydrogen bonds, and dipole-dipole interactions. In addition, the diversity of its substituents, which can be introduced through regioselective synthesis (also naturally occurring) on the coumarin core, accounts for the variety of pharmacological effects seen in many coumarin derivatives. Indeed, depending on the substituents and branching positions around the bicyclic core, coumarin-containing compounds have shown diverse pharmacological activities, ranging from anticoagulant activities to anti-inflammatory, antimicrobial, anti-HIV, and antitumor effects (Stefanachi et al., 2018). The guest editors’ interest in this core has its roots in their common doctoral studies under the supervision of Prof. Angelo Carotti at the University of Bari in taly. The main scientific results of Prof Carotti’s research group’s 20-year investigation on the coumarin core, either as a scaffold or a pharmacophore moiety, have been reported in this Research Topic (Pisani et al.).
Editorial: Coumarins: New synthetic approaches and new pharmacological applications
Stefanachi A.
;Muncipinto G.;Leonetti F.
2023-01-01
Abstract
Coumarin, a 2H-chromen-2-one oxa-heterocycle, has been extensively studied due to its occurrence in many biologically active compounds, such as Umbelliferon, the anticoagulants acenocoumarin and Warfarin, and the antibiotic Novobiocin. The ubiquity of coumarin is most likely due to its chemical structure flat, aromatic, and lipophilic with a lactone group that allows for binding to diverse targets through hydrophobic, π–π stacking, hydrogen bonds, and dipole-dipole interactions. In addition, the diversity of its substituents, which can be introduced through regioselective synthesis (also naturally occurring) on the coumarin core, accounts for the variety of pharmacological effects seen in many coumarin derivatives. Indeed, depending on the substituents and branching positions around the bicyclic core, coumarin-containing compounds have shown diverse pharmacological activities, ranging from anticoagulant activities to anti-inflammatory, antimicrobial, anti-HIV, and antitumor effects (Stefanachi et al., 2018). The guest editors’ interest in this core has its roots in their common doctoral studies under the supervision of Prof. Angelo Carotti at the University of Bari in taly. The main scientific results of Prof Carotti’s research group’s 20-year investigation on the coumarin core, either as a scaffold or a pharmacophore moiety, have been reported in this Research Topic (Pisani et al.).I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.