On July 31, 2020, Cieslikiewicz-Bouet, Monika; Naldi, Marina; Bartolini, Manuela; Perez, Belen; Servent, Denis; Jean, Ludovic; Araoz, Romulo; Renard, Pierre-Yves published an article.Application In Synthesis of 2-Amino-4-chlorobenzoic acid The title of the article was Functional characterization of multifunctional ligands targeting acetylcholinesterase and alpha 7 nicotinic acetylcholine receptor. And the article contained the following:
Alzheimer’s disease (AD) is a neurodegenerative disorder associated with cholinergic dysfunction, provoking memory loss and cognitive dysfunction in elderly patients. The cholinergic hypothesis provided over the years with mol. targets for developing palliative treatments for AD, acting on the cholinergic system, namely, acetylcholinesterase and α7 nicotinic acetylcholine receptor (α7 nAChR). In our synthetic work, we used “click-chem.” to synthesize two Multi Target Directed Ligands (MTDLs) MB105 and MB118 carrying tacrine and quinuclidine scaffolds which are known for their anticholinesterase and α7 nAChR agonist activities, resp. Both, MB105 and MB118, inhibit human acetylcholinesterase and human butyrylcholinesterase in the nanomolar range. Electrophysiol. recordings on Xenopus laevis oocytes expressing human α7 nAChR showed that MB105 and MB118 acted as partial agonists of the referred nicotinic receptor, albeit, with different potencies despite their similar structure. The different substitution at C-3 on the 2,3-disubstituted quinuclidine scaffold may account for the significantly lower potency of MB118 compared to MB105. Electrophysiol. recordings also showed that the tacrine precursor MB320 behaved as a competitive antagonist of human α7 nAChR, in the micromolar range, while the quinuclidine synthetic precursor MB099 acted as a partial agonist. Taken all together, MB105 behaved as a partial agonist of α7 nAChR at concentrations where it completely inhibited human acetylcholinesterase activity paving the way for the design of novel MTDLs for palliative treatment of AD. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Application In Synthesis of 2-Amino-4-chlorobenzoic acid
The Article related to preparation tacrine quinuclidine derivative ache nicotinic receptor, acetylcholinesterase, alpha 7 nicotinic acetylcholine receptor, alzheimer’s disease, butyrylcholinesterase, multi-target directed ligand and other aspects.Application In Synthesis of 2-Amino-4-chlorobenzoic acid
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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics