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Your search keyword '"Peltner, Lukas Klaus"' showing total 3 results
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3 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, 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

2. Discovery and Optimization of Indoline-Based Compounds as Dual 5‑LOX/sEH Inhibitors: In Vitro and In Vivo Anti-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., and Campiglia, Pietro

Published
2022
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3. Design, Synthesis, and Pharmacological Characterization of a Potent Soluble Epoxide Hydrolase Inhibitor for the Treatment of Acute Pancreatitis.

Author

Musella S, D'Avino D, Peltner LK, Di Sarno V, Cerqua I, Merciai F, Vestuto V, Ciaglia T, Smaldone G, Di Matteo F, Di Micco S, Napolitano V, Bifulco G, Pepe G, Sommella EM, Basilicata MG, Aquino G, Gomez-Monterrey IM, Campiglia P, Ostacolo C, Roviezzo F, Werz O, Rossi A, and Bertamino A

Subjects
Mice, Animals, Epoxide Hydrolases, Acute Disease, Enzyme Inhibitors therapeutic use, Enzyme Inhibitors pharmacokinetics, Pancreatitis chemically induced, Pancreatitis drug therapy
Abstract

Acute pancreatitis (AP) is a potentially life-threatening illness characterized by an exacerbated inflammatory response with limited options for pharmacological treatment. Here, we describe the rational development of a library of soluble epoxide hydrolase (sEH) inhibitors for the treatment of AP. Synthesized compounds were screened in vitro for their sEH inhibitory potency and selectivity, and the results were rationalized by means of molecular modeling studies. The most potent compounds were studied in vitro for their pharmacokinetic profile, where compound 28 emerged as a promising lead. In fact, compound 28 demonstrated a remarkable in vivo efficacy in reducing the inflammatory damage in cerulein-induced AP in mice. Targeted metabololipidomic analysis further substantiated sEH inhibition as a molecular mechanism of the compound underlying anti-AP activity in vivo . Finally, pharmacokinetic assessment demonstrated a suitable profile of 28 in vivo . Collectively, compound 28 displays strong effectiveness as sEH inhibitor with potential for pharmacological AP treatment.

Published
2023
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