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- Title
Design, Synthesis, and In Vitro Evaluation of Novel 8-Amino-Quinoline Combined with Natural Antioxidant Acids.
- Authors
Bacci, Andrea; Corsi, Francesca; Runfola, Massimiliano; Sestito, Simona; Piano, Ilaria; Manera, Clementina; Saccomanni, Giuseppe; Gargini, Claudia; Rapposelli, Simona
- Abstract
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.
- Subjects
FERULIC acid; MELANOPSIN; RETINITIS pigmentosa; NEURODEGENERATION; RETINAL diseases; OXIDATIVE stress; DRUG design
- Publication
Pharmaceuticals (14248247), 2022, Vol 15, Issue 6, p688
- ISSN
1424-8247
- Publication type
Article
- DOI
10.3390/ph15060688