Contributo in atti di convegno, 2018, ENG

Small molecules endowed with potential free radical scavenger

F. Mingoia, G. Panzeca, P. Picone, M. Di Carlo, A. Lauria

1) ISMN-CNR 2) IBIM-CNR 3) Università di Palermo, STEBICEF

The search of new small molecules behaving as free radical scavengers has attracted growing interest in drug discovery efforts because this fieldrepresents one of the most appealing therapeutic strategiesfor neuroprotection. Identifying new effective and low toxic neurotherapeutics is a challenging way for preventing neurodegeneration and mitigating against neuronal damage. A variety of central nervous system (CNS) disorders, including neurodegenerative diseases such as Alzheimer's disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis (ALS), dementia, stroke, and others, could have new therapeutic perspectives with new effective neuroprotective agents. A first step used by usfor evidencing the radical scavenger activity of the small molecules, is a DCF based assay. Further, cytocompatibility test has been performedby using different cell lines. Here, we propose our preliminary results ona structure activity relationship (SAR)of a series of variously substituted 1-Aryl-pyrazol-3-one derivatives as potential neuroprotective agents. This class of small molecules is related toEdaravone, arecentlyapproved drugfor neural damageby FDA (2017). In this way, nature and effect of substituents are under evaluationin order to get insights on the activity profile, useful for future developments.The chemical synthetic route followed involves the use of commercially available substituted reagents,providing access to a wide range of suitably substituted pyrazol-3-one derivatives.Thus, this scaffold could serve as a valuable lead for detailed SAR studies.In addition, in silico approacheswill be also considered.

Tecnologie, Ricerca di base, interdisciplinare traslazionale in ambito biomedico. Simposio IBIM-CNR/STEBICEF,, pp. 55–55, Palermo, 05/07/2018, 06/07/2018

Keywords

small molecules, radical scavenger

CNR authors

Mingoia Francesco Michele

CNR institutes

ISMN – Istituto per lo studio dei materiali nanostrutturati