Fancellu, Gaia; Chand, Karam; Tomas, Daniel; Orlandini, Elisabetta; Piemontese, Luca; Silva, Diana F.; Cardoso, Sandra M.; Chaves, Silvia; Santos, M. Amelia published an article in 2020, the title of the article was Novel tacrine-benzofuran hybrids as potential multi-target drug candidates for the treatment of Alzheimer’s Disease.Application In Synthesis of 2-Amino-4-chlorobenzoic acid And the article contains the following content:
Pursuing the widespread interest on multi-target drugs to combat Alzheimer’s disease (AD), a new series of hybrids was designed and developed based on the repositioning of the well-known acetylcholinesterase (AChE) inhibitor, tacrine (TAC), by its coupling to benzofuran (BF) derivatives The BF framework aims to endow the conjugate mols. with ability for inhibition of AChE (bimodal way) and of amyloid-beta peptide aggregation, besides providing metal (Fe, Cu) chelating ability and concomitant extra anti-oxidant activity, for the hybrids with hydroxyl substitution. The new TAC-BF conjugates showed very good activity for AChE inhibition (sub-micromolar range) and good capacity for the inhibition of self- and Cu-mediated Aβ aggregation, with dependence on the linker size and substituent groups of each main moiety. Neuroprotective effects were also found for the compounds through viability assays of neuroblastoma cells, after Aβ1-42 induced toxicity. Structure-activity relationship anal. provides insights on the best structural parameters, to take in consideration for future studies in view of potential applications in AD therapy. 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 tacrine benzofuran hybrid preparation alzheimer’s antioxidant, ache inhibitors, alzheimer’s disease, metal chelators, multi-target drugs, tacrine-benzofuran hybrids, Pharmacology: Structure-Activity and other aspects.Application In Synthesis of 2-Amino-4-chlorobenzoic acid
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