Pau, Amedeo; Catto, Marco; Pinna, Giovanni; Frau, Simona; Murineddu, Gabriele; Asproni, Battistina; Curzu, Maria M.; Pisani, Leonardo; Leonetti, Francesco; Loza, Maria Isabel; Brea, Jose; Pinna, Gerard A.; Carotti, Angelo published the artcile< Multitarget-Directed Tricyclic Pyridazinones as G Protein-Coupled Receptor Ligands and Cholinesterase Inhibitors>, Application of C8H8BrCl, the main research area is tricyclic pyridazinone GPCR ligand cholinesterase inhibitor; AChE inhibitors; BChE inhibitors; GPCR ligands; multitarget-directed ligands; neurodegenerative diseases.
By following a multitarget ligand design approach, a library of 47 compounds was prepared, and they were tested as binders of selected G protein-coupled receptors (GPCRs) and inhibitors of acetyl and/or butyryl cholinesterase. The newly designed ligands feature pyridazinone-based tricyclic scaffolds connected through alkyl chains of variable length to proper amine moieties (e.g., substituted piperazines or piperidines) for GPCR and cholinesterase (ChE) mol. recognition. The compounds were tested at three different GPCRs, namely serotoninergic 5-HT1A, adrenergic α1A, and dopaminergic D2 receptors. Our main goal was the discovery of compounds that exhibit, in addition to ChE inhibition, antagonist activity at 5-HT1A because of its involvement in neuronal deficits typical of Alzheimer’s and other neurodegenerative diseases. Ligands with nanomolar affinity for the tested GPCRs were discovered, but most of them behaved as dual antagonists of α1A and 5-HT1A receptors. Nevertheless, several compounds displaying this GPCR affinity profile also showed moderate to good inhibition of AChE and BChE, thus deserving further investigations to exploit the therapeutic potential of such unusual biol. profiles.
ChemMedChem published new progress about 5-HT1A receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Application of C8H8BrCl.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics