Search

Your search keyword '"Peltner, Lukas Klaus"' showing total 4 results
Start Over Author "Peltner, Lukas Klaus"
4 results on '"Peltner, Lukas Klaus"'

1. Design, Synthesis, and Pharmacological Characterization of a Potent Soluble Epoxide Hydrolase Inhibitor for the Treatment of Acute Pancreatitis

Author

Musella, Simona, primary, D’Avino, Danilo, additional, Peltner, Lukas Klaus, additional, Di Sarno, Veronica, additional, Cerqua, Ida, additional, Merciai, Fabrizio, additional, Vestuto, Vincenzo, additional, Ciaglia, Tania, additional, Smaldone, Gerardina, additional, Di Matteo, Francesca, additional, Di Micco, Simone, additional, Napolitano, Valeria, additional, Bifulco, Giuseppe, additional, Pepe, Giacomo, additional, Sommella, Eduardo Maria, additional, Basilicata, Manuela Giovanna, additional, Aquino, Giovanna, additional, Gomez-Monterrey, Isabel M., additional, Campiglia, Pietro, additional, Ostacolo, Carmine, additional, Roviezzo, Fiorentina, additional, Werz, Oliver, additional, Rossi, Antonietta, additional, and Bertamino, Alessia, additional

Published
2023
Full Text
View/download PDF

2. Design, Synthesis, and Pharmacological Characterization of a Potent Soluble Epoxide Hydrolase Inhibitor for the Treatment of Acute Pancreatitis

Author

Musella, Simona, D'Avino, Danilo, Peltner, Lukas Klaus, Di Sarno, Veronica, Cerqua, Ida, Merciai, Fabrizio, Vestuto, Vincenzo, Ciaglia, Tania, Smaldone, Gerardina, Di Matteo, Francesca, Di Micco, Simone, Napolitano, Valeria, Bifulco, Giuseppe, Pepe, Giacomo, Sommella, Eduardo Maria, Basilicata, Manuela Giovanna, Aquino, Giovanna, Gomez-Monterrey, Isabel M, Campiglia, Pietro, Ostacolo, Carmine, Roviezzo, Fiorentina, Werz, Oliver, Rossi, Antonietta, and Bertamino, Alessia

Published
2023

3. Discovery and Optimization of Indoline-Based Compounds as Dual 5-LOX/sEH Inhibitors: In Vitro and In Vivo Anti-Inflammatory Characterization

Author

Cerqua, Ida, primary, Musella, Simona, additional, Peltner, Lukas Klaus, additional, D’Avino, Danilo, additional, Di Sarno, Veronica, additional, Granato, Elisabetta, additional, Vestuto, Vincenzo, additional, Di Matteo, Rita, additional, Pace, Simona, additional, Ciaglia, Tania, additional, Bilancia, Rossella, additional, Smaldone, Gerardina, additional, Di Matteo, Francesca, additional, Di Micco, Simone, additional, Bifulco, Giuseppe, additional, Pepe, Giacomo, additional, Basilicata, Manuela Giovanna, additional, Rodriquez, Manuela, additional, Gomez-Monterrey, Isabel M., additional, Campiglia, Pietro, additional, Ostacolo, Carmine, additional, Roviezzo, Fiorentina, additional, Werz, Oliver, additional, Rossi, Antonietta, additional, and Bertamino, Alessia, additional

Published
2022
Full Text
View/download PDF

4. Discovery and Optimization of Indoline-Based Compounds as Dual 5-LOX/sEH Inhibitors: In Vitroand In VivoAnti-Inflammatory Characterization

Author

Cerqua, Ida, Musella, Simona, Peltner, Lukas Klaus, D’Avino, Danilo, Di Sarno, Veronica, Granato, Elisabetta, Vestuto, Vincenzo, Di Matteo, Rita, Pace, Simona, Ciaglia, Tania, Bilancia, Rossella, Smaldone, Gerardina, Di Matteo, Francesca, Di Micco, Simone, Bifulco, Giuseppe, Pepe, Giacomo, Basilicata, Manuela Giovanna, Rodriquez, Manuela, Gomez-Monterrey, Isabel M., Campiglia, Pietro, Ostacolo, Carmine, Roviezzo, Fiorentina, Werz, Oliver, Rossi, Antonietta, and Bertamino, Alessia

Abstract

The design of multitarget drugs represents a promising strategy in medicinal chemistry and seems particularly suitable for the discovery of anti-inflammatory drugs. Here, we describe the identification of an indoline-based compound inhibiting both 5-lipoxygenase (5-LOX) and soluble epoxide hydrolase (sEH). In silicoanalysis of an in-house library identified nine compounds as potential 5-LOX inhibitors. Enzymatic and cellular assays revealed the indoline derivative 43as a notable 5-LOX inhibitor, guiding the design of new analogues. These compounds underwent extensive in vitroinvestigation revealing dual 5-LOX/sEH inhibitors, with 73showing the most promising activity (IC50s of 0.41 ± 0.01 and 0.43 ± 0.10 μM for 5-LOX and sEH, respectively). When challenged in vivo in zymosan-induced peritonitis and experimental asthma in mice, compound 73showed 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.

Published
2022
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results