Indoloquinoxaline derivatives as promising multi-functional anti-Alzheimer agents

Kanhed, Ashish M.; Patel, Dushyant V.; Patel, N. K.; Sinha, Anshuman; Thakor, Priyanka S; Patel, Kishan B; Prajapati, Navnit; Patel, Kirti; Yadav, Mange Ram

doi:10.1080/07391102.2020.1840441

Cited by 16 publications

(10 citation statements)

References 52 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The synthesized compounds exhibited modest to good AChE inhibitory activity. The most active compound in this series inhibits the self-induced A β 1–42 aggregation and possesses antioxidant activity [ 64 ].…”

Section: Phenolic Acids-based Hybridsmentioning

confidence: 99%

Antioxidant Compounds in the Treatment of Alzheimer’s Disease: Natural, Hybrid, and Synthetic Products

Hatami

Mortazavi

Baseri

et al. 2023

Evidence-Based Complementary and Alternative Medicine

View full text Add to dashboard Cite

Alzheimer’s disease (AD) which is associated with cognitive dysfunction and memory lapse has become a health concern. Various targets and pathways have been involved in AD’s progress, such as deficit of acetylcholine (ACh), oxidative stress, inflammation, β-amyloid (Aβ) deposits, and biometal dyshomeostasis. Multiple pieces of evidence indicate that stress oxidative participation in an early stage of AD and the generated ROS could enable neurodegenerative disease leading to neuronal cell death. Hence, antioxidant therapies are applied in treating AD as a beneficial strategy. This review refers to the development and use of antioxidant compounds based on natural products, hybrid designs, and synthetic compounds. The results of using these antioxidant compounds were discussed with the given examples, and future directions for the development of antioxidants were evaluated.

show abstract

Section: Phenolic Acids-based Hybridsmentioning

confidence: 99%

Antioxidant Compounds in the Treatment of Alzheimer’s Disease: Natural, Hybrid, and Synthetic Products

Hatami

Mortazavi

Baseri

et al. 2023

Evidence-Based Complementary and Alternative Medicine

View full text Add to dashboard Cite

show abstract

“…The amkapine CX516 has the quinoxaline structure linked to benzyl piperidine [57]. Quinoxaline nucleus fused with indole, thiazole, and their derivatives were found to inhibit acetylcholinesterase [58,59].…”

Section: Introductionmentioning

confidence: 99%

2d Qsar and Docking Studies on Chalcone - Quinoxaline Variants – a Potential Target for Acetylcholinestrase Inhibitors

VELMURUGAN¹,

Sivaraman²,

Natarajan³

2023

Preprint

View full text Add to dashboard Cite

The Quantitative Structural Activity Relationship among 49 reported compounds containing chalcone derivatives as an acetylcholinesterase inhibitor. The acetylcholinesterase enzyme is the major leading threat to neurodegenerative disorders. The 2D QSAR study was done using QSARINS software. Model 2 was obtained as the best model with an r2 value of 0.9398. The OECD principles were used to validate the model. The applicability domain of the model resulted in zero outliers. Based on the results of the QSAR study, 10 novel ligands possessing chalcones fused with quinoxaline were drawn. These 10 novel ligands showed class 5 toxicity, which was predicted using PROTOX II software. The ADME properties were also screened using preADMET. Molecular docking was performed between the 10 ligands and the acetylcholinesterase enzyme (PDB ID: 4EY7) using Autodock 4.0 softaware. 2D visualisation of drug interactions was also discussed. Compounds 4 and 5 with substitution of p-chloro and 2-bromo respectively demonstrated active binding to the catalytic anionic site and the peripheral anionic site, respectively. These results were compared with those of the standard drug, donepezil.

show abstract

“…[4] Likewise, it has been recently demonstrated that indoloquinoxaline deriva-tives appear to be promising multi-functional agents for the treatment of Alzheimer's disease. [5] Nevertheless, compound B-220 appears to be the most illustrious indoloquinoxaline derivative, which is considered a promising antiherpesvirus agent. [6] Despite the existence of various approaches to the construction of indolopyrazine scaffold, the most famous preparation method of these compounds consist of the condensation of isatin with phenylenediamine derivatives.…”

Section: Introductionmentioning

confidence: 99%

“…More interestingly, the indolo[2,3‐ b ]quinoxaline scaffold is a part of an essential diversity of DNA intercalating agents endowed with many pharmacological activities such as various antiviral, [2] anticancer, [3] and antidiabetic activities [4] . Likewise, it has been recently demonstrated that indoloquinoxaline derivatives appear to be promising multi‐functional agents for the treatment of Alzheimer′s disease [5] …”

Section: Introductionmentioning

confidence: 99%

New Approach to Biologically Active Indolo[2,3‐b]quinoxaline Derivatives through Intramolecular Oxidative Cyclodehydrogenation

Verbitskiy

2022

ChemistrySelect

View full text Add to dashboard Cite

A convenient synthetic protocol to antiviral agent B‐220 and a series of similar indolo[2,3‐b]quinoxaline derivatives has been developed. This synthetic approach is based on Buchwald‐Hartwig cross‐coupling and subsequent annulation by intramolecular oxidative cyclodehydrogenation. For the first time, 6H‐indolo[2,3‐b]quinoxaline amine derivatives were evaluated for antimycobacterial activity. The moderate bacteriostatic effect against Mycobacterium tuberculosis H37Rv was found. A plausible mechanism of antibacterial action was elucidated by the molecular docking.

show abstract

Indoloquinoxaline derivatives as promising multi-functional anti-Alzheimer agents

Cited by 16 publications

References 52 publications

Antioxidant Compounds in the Treatment of Alzheimer’s Disease: Natural, Hybrid, and Synthetic Products

Antioxidant Compounds in the Treatment of Alzheimer’s Disease: Natural, Hybrid, and Synthetic Products

2d Qsar and Docking Studies on Chalcone - Quinoxaline Variants – a Potential Target for Acetylcholinestrase Inhibitors

New Approach to Biologically Active Indolo[2,3‐b]quinoxaline Derivatives through Intramolecular Oxidative Cyclodehydrogenation

Contact Info

Product

Resources

About