Design, synthesis and biological evaluation of multifunctional tacrine-curcumin hybrids as new cholinesterase inhibitors with metal ions-chelating and neuroprotective property was written by Liu, Zhikun;Fang, Lei;Zhang, Huan;Gou, Shaohua;Chen, Li. And the article was included in Bioorganic & Medicinal Chemistry in 2017.Recommanded Product: Ethyl 2-(2-methyl-1,3-dioxolan-2-yl)acetate The following contents are mentioned in the article:
Total sixteen tacrine-curcumin hybrid compounds were designed and synthesized for the purpose of searching for multifunctional anti-Alzheimer agents. In vitro studies showed that these hybrid compounds showed good cholinesterase inhibitory activity. Particularly, the potency of K3-2 is even beyond tacrine. Some of the compounds exhibited different selectivity on acetylcholinesterase or butyrylcholinesterase due to the structural difference. Thus, the structure and activity relationship is summarized and further discussed based on mol. modeling studies. The ORAC and MTT assays indicated that the hybrid compounds possessed pronounced antioxidant activity and could effectively protect PC12 cells from the H2O2/Aβ42-induced toxicity. Moreover, the hybrid compounds also showed pos. metal ions-chelating ability in vitro, suggesting a potential to halt ion-induced Aβ aggregation. All the obtained results demonstrated that the tacrine-curcumin hybrid compounds, in particular compound K3-2, can be considered as potential therapeutic agents for Alzheimer’s disease. This study involved multiple reactions and reactants, such as Ethyl 2-(2-methyl-1,3-dioxolan-2-yl)acetate (cas: 6413-10-1Recommanded Product: Ethyl 2-(2-methyl-1,3-dioxolan-2-yl)acetate).
Ethyl 2-(2-methyl-1,3-dioxolan-2-yl)acetate (cas: 6413-10-1) belongs to dioxole derivatives. Dioxoles, particularly fluorinated dioxoles, are used as co-monomers to make polymers that find use in forming protective coatings for chemical resistance. Although benzodioxole is not particularly important, many related compounds containing the methylenedioxyphenyl group are bioactive, and thus are found in pesticides and pharmaceuticals.Recommanded Product: Ethyl 2-(2-methyl-1,3-dioxolan-2-yl)acetate
Referemce:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem