54402-13-0Relevant articles and documents
Benzofuran-derived benzylpyridinium bromides as potent acetylcholinesterase inhibitors
Baharloo, Farzaneh,Moslemin, Mohammad Hossein,Nadri, Hamid,Asadipour, Ali,Mahdavi, Mohammad,Emami, Saeed,Firoozpour, Loghman,Mohebat, Razieh,Shafiee, Abbas,Foroumadi, Alireza
, p. 196 - 201 (2015)
A series of benzofuran-based N-benzylpyridinium derivatives 5a-o were designed and synthesized as novel AChE inhibitors. The synthetic pathway of the compounds involved the preparation of 4-(benzofuran-2-yl)pyridine intermediates via the reaction of different salicylaldehyde derivatives and 4-(bromomethyl)pyridine, followed by intramolecular cyclization. Subsequently, the 4-(benzofuran-2-yl)pyridines were N-benzylated by using appropriate benzyl bromide to afford the final product 5a-o. The results of in vitro AChE activity evaluation of synthesized compounds revealed that all compound had potent anti-AChE activity comparable or more potent than standard drug donepezil. The N-(3,5-dimethylbenzyl) derivative 5e with IC50 value of 4.1 nM was the most active compound, being 7-fold more potent than donepezil.
Bronsted acid catalyzed intramolecular benzylic cyclizations of alkylpyridines
Lansakara, Ashabha I.,Farrell, Daniel P.,Pigge, F. Christopher
supporting information, p. 1090 - 1099 (2014/02/14)
Aldehyde and ketone electrophiles incorporated into the side chains of 2- and 4-alkylpyridines participate in intramolecular aldol-like condensations with pyridine benzylic carbons in the presence of Bronsted acid catalysts. Pyridines featuring β-ketoamid
Histidine-(N-benzyl glycinamide) inhibitors of protein farnesyl transferase
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, (2008/06/13)
Inhibitors of protein farnesyl transferase enzymes are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating cancer, restenosis, psoriasis, endometriosis, atherosclerosis, or viral infe