Synthesis and acetyl cholinesterase inhibitory activity of new oxazole, 1, 2, 4 - triazole derivatives bearing carbamazepine as nucleus

Cadaba indica, a component of traditional siddha medicine, is used for the therapy of gonorrhea, inflammation, eczema etc. The present study shows that it exhibited acetylcholinesterase inhibitory activity (up to 81.5 ± 1.5%) at the concentration of 3 mg/mL, with the IC50 value of 1.8 mg/mL. Furthermore, the ethanol extract of C. indica therapy at a dose of 100 mg/kg p.o significantly ameliorated the cognitive impaired mice in Y-maze task. The active ingredient was identified as 3,3’,4’,5,7-pentahydroxyflavone. The above results suggest that C. indica would be a potential natural therapeutic remedy for cognitive disorders mediated by cholinergic dysfunction.Video Clip:<a href="https://youtube.com/v/QIEuwPT-lmw">Memory impairment test in mice</a>: 1 min

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7-Amine-spiro[chromeno[4,3-b]quinoline-6,1′-cycloalkanes]: Synthesis and cholinesterase inhibitory activity of structurally modified tacrines

Bioorganic Chemistry ◽

10.1016/j.bioorg.2021.104649 ◽

2021 ◽

Vol 108 ◽

pp. 104649 ◽

Cited By ~ 1

Author(s):

Letícia B. Silva ◽

Pablo A. Nogara ◽

Paula T. Halmenschelager ◽

Jéssica C. Alvim ◽

Fernanda D'A. Silva ◽

...

Keyword(s):

Inhibitory Activity ◽

Cholinesterase Inhibitory Activity

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Discovery of antiproliferative and anti-FAK inhibitory activity of 1,2,4-triazole derivatives containing acetamido carboxylic acid skeleton

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2021.127965 ◽

2021 ◽

pp. 127965

Author(s):

Muhamad Mustafa ◽

Gamal El-Din A. Abuo-Rahma ◽

Amer Ali Abd El-Hafeez ◽

Esam R. Ahmed ◽

Dalia Abdelhamid ◽

...

Keyword(s):

Carboxylic Acid ◽

Inhibitory Activity ◽

Triazole Derivatives

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Bioassay-Guided Isolation and Identification of a Acetylcholinesterase Inhibitors from Calophyllum polyanthum

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.634-638.1225 ◽

2013 ◽

Vol 634-638 ◽

pp. 1225-1228 ◽

Cited By ~ 1

Author(s):

Fei Zhang ◽

Hai Wei Ren ◽

Yong Gang Wang ◽

Rong Wang ◽

Jie Sheng

Keyword(s):

Inhibitory Activity ◽

Cholinesterase Activity ◽

Spectral Characteristics ◽

Ethanolic Extract ◽

Acetylcholinesterase Inhibitors ◽

Microplate Assay ◽

Acetyl Cholinesterase ◽

Isolation And Identification ◽

Active Compounds ◽

Bioautographic Method

A significant acetylcholinesterase inhibitory activity was observed for the Ethanolic extract from the leaves of Calophyllum polyanthum by using TLC bioautographic method. Further bioassay-guided isolation of this extract using TLC bioautographic method resulted in obtaining a pyranochromanone, apetalic acid (1). The structure of 1 was identified by comparison of it’s spectral characteristics with previous reports. The concentration required for 50% inhibition of 1 was 0.95 mM, determined by a microplate assay. The anti-acetylcholinesterase aity of compound 1 was weak, but it was the first pyranochromanone which have anti-acetyl cholinesterase activity. As a new leading compound, it can be modified and transformed to obtain more potently active compounds.

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Isolation and Cholinesterase Inhibitory Activity of Narcissus Extracts and Amaryllidaceae Alkaloid

Natural Product Communications ◽

10.1177/1934578x1300800625 ◽

2013 ◽

Vol 8 (6) ◽

pp. 1934578X1300800 ◽

Cited By ~ 2

Author(s):

Lucie Cahlíková ◽

Miroslav Ločárek ◽

Nina Benešová ◽

Radim Kučera ◽

Jakub Chlebek ◽

...

Keyword(s):

Biological Activity ◽

Inhibitory Activity ◽

Mass Spectra ◽

Dependent Manner ◽

Inhibition Activity ◽

Narcissus Poeticus ◽

Cholinesterase Inhibitory Activity ◽

Alkaloid Extracts ◽

Dose Dependent ◽

Retention Indexes

Alkaloid extracts of eleven Narcissus (Amaryllidaceae) species and varieties were studied with respect to their acetylcholinesterase (HuAChE) and butyrylcholinesterase (HuBuChE) inhibitory activity and alkaloid patterns. Forty-two alkaloids were determined by GC/MS, and thirty of them identified from their mass spectra, retention times and retention indexes. Promising HuAChE inhibition activity was demonstrated by nine Narcissus taxa and HuBuChE inhibition by Narcissus poeticus cv. Pink Parasol with an IC50 value of 3.3 ± 0.5 μg/mL. The alkaloid identified as (11C- S)-homolycorine was isolated in pure form from Narcissus Sir W. Churchill using preparative TLC and was tested for its biological activity. Homolycorine inhibited HuAChE and HuBuChE in a dose-dependent manner with IC50 values of 63.7±4.3 μM and 151.0±15.2 μM, respectively.

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