Design, Synthesis, and In Vitro Evaluation of Novel 8-Amino-Quinoline Combined with Natural Antioxidant Acids

Autor: Andrea Bacci, Francesca Corsi, Massimiliano Runfola, Simona Sestito, Ilaria Piano, Clementina Manera, Giuseppe Saccomanni, Claudia Gargini, Simona Rapposelli
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: Pharmaceuticals, Vol 15, Iss 6, p 688 (2022)
Druh dokumentu: article
ISSN: 1424-8247
DOI: 10.3390/ph15060688
Popis: Overproduction of reactive oxygen species (ROS) and alterations in metallostasis are common and related hallmarks in several neurodegenerative diseases (NDDs). Nature-based derivatives always represent an attractive tool in MTDL drug design, especially against ROS in NDDs. On this notion, we designed a new series of 8-quinoline-N-substituted derivatives with a natural antioxidant portion (i.e., lipoic, caffeic, and ferulic acids). These compounds were shown to chelate copper, a metal involved in ROS-induced degeneration, and scavenger oxygen radicals in DPPH assay. Then, selected compounds 4 and 5 were evaluated in an in vitro model of oxidative stress and shown to possess cytoprotective effects in 661W photoreceptor-like cells. The obtained results may represent a starting point for the application of the proposed class of compounds in retinal neurodegenerative diseases such as retinitis pigmentosa (RP), comprising a group of hereditary rod–cone dystrophies that represent a major cause of blindness in patients of working age, where the progression of the disease is a multifactorial event, with oxidative stress contributing predominantly.
Databáze: Directory of Open Access Journals
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