Coumarin derivatives as potential inhibitors of acetylcholinesterase: Synthesis, molecular docking and biological studies

Singla, Sumit; Piplani, Poonam

doi:10.1016/j.bmc.2016.07.061

Cited by 32 publications

(17 citation statements)

References 42 publications

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“…al., 2016). According to Singhla and Piplani (2016) [39], a synthesized coumarin related compound displayed significant antiamnesic activity, antioxidant activity in comparison to donepezil and AChE inhibitory activity.…”

Section: Discussionmentioning

confidence: 99%

GC/MS analysis and In-vitro Antioxidant activity of methanol extract of Ulothrix flacca and its main constituent Dimethyl Sulfone.

Vasudevarao¹,

Sravanthi²

2017

IOSRJPBS

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Section: Discussionmentioning

confidence: 99%

GC/MS analysis and In-vitro Antioxidant activity of methanol extract of Ulothrix flacca and its main constituent Dimethyl Sulfone.

Vasudevarao¹,

Sravanthi²

2017

IOSRJPBS

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“…It should be mentioned that among the developed various pharmaceuticals as AChE inhibitors such as donepezil, rivastigmine, galantamine, ensaculine, and propidium, and tacrine, there is at least one drug, namely ensaculine, which encompasses the coumarin in its structure. Moreover, several reports demonstrate the inhibitory effects of coumarins against AChE . In the present work, 14 coumarins were evaluated for their AChE inhibitory effects.…”

Section: Acetylcholinesterase Inhibition Assaymentioning

confidence: 96%

“…Coumarins (2 H ‐chromen‐2‐one) are important heterocyclic compounds which consist of fused benzene and α‐pyrone rings (Scheme ). Both of synthetic and natural coumarins are valuable structures in drug design and development, due to broad spectrum of biological properties including anti‐HIV, antimicrobial, anticancer, anti‐inflammatory, anti‐Alzheimer, and antidepressant activities. Several well‐known natural and synthetic drugs with the core structure of coumarin are used clinically (Scheme ).…”

Section: Introductionmentioning

confidence: 99%

Rapid, Efficient, and Green Synthesis of Coumarin Derivatives via Knoevenagel Condensation and Investigating Their Biological Effects

et al. 2019

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Coumarins as naturally occurring heterocycles are chemically and biologically attractive compounds due to their diverse pharmacological properties. This study aimed to design a green method for the synthesis of coumarin derivatives followed by their biological investigations. To do so, coumarins were synthesized with excellent yields using a one-pot procedure under solvent-free conditions at room temperature with very short reaction times. 1-hexyl-3-methylimidazolium bromide was used as a reaction medium and an alternative for common toxic solvents. The structure of coumarins was confirmed using spectroscopic techniques as well as elemental analysis. The cytotoxicity of coumarins was evaluated against A549 cancerous cells and was found to be non-cytotoxic in nature. Also, their abilities for inhibition of acetylcholinesterase, tyrosinase, and α-glucosidase were assessed. The results showed that some derivatives have mild to moderate inhibitory activity (IC 50 = 3.64-5.96 mm) against acetylcholinesterase. The tested coumarins have also moderately inhibited tyrosinase (IC 50 = 3.95-13.96 mm). The results of this study could be useful for the design and development of green and effective methods for the synthesis of new drugs with the core structure of coumarin.

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“…The synthesis of different AChE inhibitor derivatives or hybrid molecules has attracted attention in recent years (for example, piperidine de-rivatives [23], tetrazole derivatives [3], hydroxyquinoline derivatives [24], isoquinolines [25], carbamate derivatives [26], β-lactam analogs and Schiff bases [from 2-naphtaldehyde and substituted aniline derivatives] [27], and coumarin derivatives [28]). Because tacrine is a well-known cholinesterase inhibitor for the treatment of AD, researchers have focused on the development of more active and selective ligands than unmodified tacrine.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of novel Schiff base derivatives of tacrine and investigation of their acetylcholinesterase inhibition potency

Koyuncu

Yaşar

Arslan

et al. 2019

Maced. J. Chem. Chem. Eng.

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Investigation of acetylcholinesterase (AChE) inhibition potency of some new Schiff base derivatives of tacrine (9-amino-1,2,3,4-tetrahydroacridine) was reported in this paper. Novel Schiff base derivatives of tacrine (3a–g) have been synthesized, and they have been characterized by several methods (FT-IR, 1H-NMR, 13C-NMR, etc.). Then, inhibition effects on AChE by the synthesized compounds have been investigated by the spectrophotometric Ellman method. IC50, Ki, KM and Vmax values and inhibition types have been determined. It was seen that all compounds had the property of a water-soluble reversible AChE inhibitor. Structure 3a was found to be the most potent inhibitor, with the IC50 value of 22.1 ± 1.11 nM (tacrine's IC50 value was calculated as 34.1 nM).

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Coumarin derivatives as potential inhibitors of acetylcholinesterase: Synthesis, molecular docking and biological studies

Cited by 32 publications

References 42 publications

GC/MS analysis and In-vitro Antioxidant activity of methanol extract of Ulothrix flacca and its main constituent Dimethyl Sulfone.

GC/MS analysis and In-vitro Antioxidant activity of methanol extract of Ulothrix flacca and its main constituent Dimethyl Sulfone.

Rapid, Efficient, and Green Synthesis of Coumarin Derivatives via Knoevenagel Condensation and Investigating Their Biological Effects

Synthesis of novel Schiff base derivatives of tacrine and investigation of their acetylcholinesterase inhibition potency

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