Discovery and Optimization of Indoline-Based Compounds as Dual 5-LOX/sEH Inhibitors: <i>In Vitro</i> and <i>In Vivo</i> Anti-Inflammatory Characterization
Ida Cerqua, Simona Musella, Lukas K. Peltner, Danilo D’Avino, Veronica Di Sarno, Elisabetta Granato, Vincenzo Vestuto, Rita Di Matteo, Simona Pace, Tania Ciaglia, Rossella Bilancia, Gerardina Smaldone, Francesca Di Matteo, Simone Di Micco, Giuseppe Bifulco, Giacomo Pepe, Manuela Giovanna Basilicata, Manuela Rodriquez, Isabel Gómez‐Monterrey, Pietro Campiglia, Carmine Ostacolo, Fiorentina Roviezzo, Oliver Werz, Antonietta Rossi, Alessia Bertamino
Abstract
showed remarkable anti-inflammatory efficacy. These results pave the way for the rational design of 5-LOX/sEH dual inhibitors and for further investigation of their potential use as anti-inflammatory agents.
Topics & Concepts
ChemistryEpoxide hydrolase 2IndolineIn vivoIn silicoIn vitroPharmacologyPharmacophoreStructure–activity relationshipIn vitro toxicologyZymosanArachidonate 5-lipoxygenaseEnzymeBiochemistryStereochemistryMedicineGeneArachidonic acidBiologyBiotechnologyEicosanoids and Hypertension PharmacologyInflammatory mediators and NSAID effectsFree Radicals and Antioxidants