Therapeutic potential of quinazoline derivatives for Alzheimer's disease: A comprehensive review

Haghighijoo, Zahra; Zamani, Leila; Moosavi, Fatemeh; Emami, Saeed

doi:10.1016/j.ejmech.2021.113949

Cited by 36 publications

(22 citation statements)

References 219 publications

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“…In the discovery and design of innovative CNS-active medications, the quinazoline scaffold is critical. Quinazolines drug-like properties and pharmacological abilities could result in a wide range of drugs with a wide range of targets (Haghighijoo et al, 2022). Alzheimer's disease (AD) is a neurodegenerative illness that affects impairment of memory, cognitive impairment, and language difficulties.…”

Section: Anti-alzheimer Quinazolinesmentioning

confidence: 99%

A comprehensive review of recent advances in the biological activities of quinazolines

Gomaa

2022

Chem Biol Drug Des

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Quinazoline heterocycles are critical in the development of medications.Quinazoline derivatives have been intensively researched, providing a wide range of compounds with diverse biological roles. The quinazoline nucleus has garnered a lot of attention in medical chemistry in recent years. It was assumed to be a pharmacophore component in the development of physiologically interesting drugs. This review is an attempt to increase the potential of quinazoline by highlighting a wide range of advancements demonstrated by numerous derivatives of the quinazoline moiety, as well as focusing on diverse pharmacological actions of the quinazoline moiety. This review compiles recent studies on the quinazoline moiety described in the literature by researchers.

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Section: Anti-alzheimer Quinazolinesmentioning

confidence: 99%

A comprehensive review of recent advances in the biological activities of quinazolines

Gomaa

2022

Chem Biol Drug Des

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“…Quinazoline-fused heterocyclic derivatives are important members of the N-heterocycle family, which have aroused considerable attention due to their important biopharmaceutical properties. 8 In the same year, Jeong et al 9 reported the cyclization reaction of 1 H -indazol-3-amine, 4-fluoro-1 H -indazol-3-amine, 5-bromo-1 H -indazol-3-amine or 6-fluoro-1 H -indazol-3-amine with aldehydes and cyclic 1,3-dicarbonyl compounds to obtain tetrahydroindazolo[3,2- b ]quinazoline derivatives (Scheme 6). The optimized conditions were established as using FeF 3 as the catalyst at 80 °C with ultrasonication under solvent-free conditions, which resulted in excellent yields.…”

Section: Condensation Annulation Of 3-aminoindazolesmentioning

confidence: 99%

Recent advances in 3-aminoindazoles as versatile synthons for the synthesis of nitrogen heterocycles

Guo

Gao

2022

Org. Biomol. Chem.

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“…Alzheimer’s disease (AD) is a progressive and irreversible neurodegenerative disorder that slowly results in the state of dementia [ 1 , 2 ]. Several theories have been proposed to explain the root cause of AD, whilst the exact mechanism is still under debate [ 3 , 4 ].…”

Section: Introductionmentioning

confidence: 99%

In Silico Drug Design and Analysis of Dual Amyloid-Beta and Tau Protein-Aggregation Inhibitors for Alzheimer’s Disease Treatment

2023

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Alzheimer’s disease (AD) is a progressive and irreversible neurodegenerative disorder that gradually leads to the state of dementia. The main features of AD include the deposition of amyloid-beta peptides (Aβ), forming senile plaques, and the development of neurofibrillary tangles due to the accumulation of hyperphosphorylated Tau protein (p-tau) within the brain cells. In this report, seven dual-inhibitor molecules (L1–7) that can prevent the aggregation of both Aβ and p-tau are suggested. The drug-like features and identification of the target proteins are analyzed by the in silico method. L1–7 show positive results in both Blood–Brain Barrier (BBB) crossing and gastrointestinal absorption, rendering to the results of the permeation method. The molecular docking test performed for L1–7 shows binding energies in the range of −4.9 to −6.0 kcal/mol towards Aβ, and −4.6 to −5.6 kcal/mol for p-tau. The drug’s effectiveness under physiological conditions is assessed by the use of solvation models on the investigated systems. Further, the photophysical properties of L1–3 are predicted using TD-DFT studies.

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Therapeutic potential of quinazoline derivatives for Alzheimer's disease: A comprehensive review

Cited by 36 publications

References 219 publications

A comprehensive review of recent advances in the biological activities of quinazolines

A comprehensive review of recent advances in the biological activities of quinazolines

Recent advances in 3-aminoindazoles as versatile synthons for the synthesis of nitrogen heterocycles

In Silico Drug Design and Analysis of Dual Amyloid-Beta and Tau Protein-Aggregation Inhibitors for Alzheimer’s Disease Treatment

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