Design, synthesis and pharmacological evaluation of novel tacrine–caffeic acid hybrids as multi-targeted compounds against Alzheimer’s disease

Design, synthesis and neuroprotective evaluation of novel tacrine–benzothiazole hybrids as multi-targeted compounds against Alzheimer’s disease

“…The presence of fibrils can be monitored by the fluorescence emission of ThT, with the absorption peak at 446 nm and the emission peak at 490 nm. [39][40][41] The inhibition studies were carried out upon incubating Aβ 42 with and without the compounds. The results (summarized in Table 1) show that all the compounds induced the decrease of the ThT fluorescence that was associated with the Aβ fibril binding, thus inhibited the Aβ 42 self-aggregation process.…”

Synthesis, biological activity, and biopharmaceutical characterization of tacrine dimers as acetylcholinesterase inhibitors

“…Over the past decade, various THA derivatives have been developed and indeed demonstrated multi-target properties in vitro and in animal models, including inhibition of AChE, BACE1, Ab aggregation and reactive oxygen species as well as blockade of NMDA receptor and nitric oxide synthase, etc. (Alcala Mdel et al, 2003;Alonso et al, 2005;Chao et al, 2012;Fu et al, 2007Fu et al, , 2008Li et al, 2006;Minarini et al, 2012;Pi et al, 2012). Bis(7)-tacrine (B7T), a dimeric THA analog designed with the aid of computer docking program and synthesized by our research group (Fig.…”

Tacrine-allyl/propargylcysteine–benzothiazole trihybrids as potential anti-Alzheimer's drug candidates

“…15 The assay solution contained 374 tL of Hepes buffer (50 mM and pH8.0), a variable volume (10- To study the A342 aggregation inhibition, a reported method, based on the fluorescence emission of thioflavin T (ThT), was followed. 16,28,29 It is based on the assumption that …”

“…The presence of fibrils can be monitored by the fluorescence emission of ThT, with the absorption peak at 446 nm and the emission peak at 485 nm. 28,29,30 The inhibition studies were carried out upon incubating A342 in the presence and absence of the ligands. The results, summarized in Table S1) 19 or tacrine itself, showed a general increase of up to 5-fold the percentage of inhibition for the same experimental conditions, which is clearly attributed to the further inclusion of the BTA moiety in these hybrids.…”