New thiazole and thiazole-chromene hybrids possessing morpholine units: Piperazine-mediated one-pot synthesis of potential acetylcholinesterase inhibitors
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https://doi.org/10.1080/00397911.2021.1970774
Document Type
Research Article
Publication Title
Synthetic Communications
Publication Date
1-1-2021
doi
10.1080/00397911.2021.1970774
Abstract
In the current study, new morpholine-linked thiazoles were prepared by the reaction of salicylaldehyde derivative, thiosemicarbazide, and α-bromoketones. To mediate the previous three-component reaction, the reaction was conducted using two equiv. of piperazine in dioxane at reflux for 5 h. Using the prior protocol, two series of thiazoles, linked to arene or chromene units, were prepared in good to excellent yields. The new thiazoles were examined as potential inhibitors of acetylcholinesterase at a concentration of 50 µM. When compared to donepezil (inhibition percentage of 92.8%), hybrids 11b and 11c, linked to 6-chloro or 6-bromochromen-3-yl units, gave the best inhibition percentages of 72.3 and 71.5%, respectively. Furthermore, when tested at a concentration of 25 µg/mL, the same hybrids demonstrated the highest DPPH antioxidant activity, with inhibition percentages of 84.1 and 83.2%, respectively, when compared to ascorbic acid (inhibition percentage of 89.5%).
First Page
3332
Last Page
3344
Recommended Citation
APA Citation
Mekky, A.
Sanad, S.
&
El-Idreesy, T.
(2021). New thiazole and thiazole-chromene hybrids possessing morpholine units: Piperazine-mediated one-pot synthesis of potential acetylcholinesterase inhibitors. Synthetic Communications, 51(21), 3332–3344.
10.1080/00397911.2021.1970774
https://fount.aucegypt.edu/faculty_journal_articles/2681
MLA Citation
Mekky, Ahmed E.M., et al.
"New thiazole and thiazole-chromene hybrids possessing morpholine units: Piperazine-mediated one-pot synthesis of potential acetylcholinesterase inhibitors." Synthetic Communications, vol. 51,no. 21, 2021, pp. 3332–3344.
https://fount.aucegypt.edu/faculty_journal_articles/2681