Design, synthesis, and biological evaluation of thienopyrimidine derivatives as multifunctional agents against Alzheimer's disease

KI Eissa, MM Kamel, LW Mohamed… - Drug Development …, 2023 - Wiley Online Library
A series of 12 S‐substituted tetrahydrobenzothienopyrimidines were designed and
synthesized based on the donepezil scaffold. All the newly synthesized compounds were …

Development of new Alzheimer's disease drug candidates using donepezil as a key model

KI Eissa, MM Kamel, LW Mohamed… - Archiv der …, 2023 - Wiley Online Library
Alzheimer's disease (AD) is one of the most prevalent geriatric diseases and a significant
cause of high mortality. This crippling disorder is becoming more prevalent at an …

Multidisciplinary approaches for advanced enzyme biocatalysis in pharmaceuticals: protein engineering, computational biology, and nanoarchitectonics

S Kim, S Ga, H Bae, R Sluyter, K Konstantinov… - EES Catalysis, 2023 - pubs.rsc.org
Enzyme biocatalysis is reshaping pharmaceutical synthesis, offering sustainable and
efficient pathways for drug discovery and production. This paradigm shift towards eco …

New indole derivatives as multitarget anti-Alzheimer's agents: synthesis, biological evaluation and molecular dynamics

EM Azmy, IF Nassar, M Hagras, IM Fawzy… - Future Medicinal …, 2023 - Taylor & Francis
Background: Alzheimer's disease is a neurological disorder that causes brain cells to shrink
and die. Aim: Thirteen novel 'oxathiolanyl','pyrazolyl'and 'pyrimidinyl'indole derivatives were …

Synthesis and Evaluation of Acetylcholinesterase Inhibitory and Cytotoxic Activities of Pyrano[2,3-d]pyrimidines

NH Thanh, NTQ Giang, NV Ha… - Natural Product …, 2023 - journals.sagepub.com
Objective: The study was conducted to evaluate the in vitro acetylcholinesterase (AchE)
inhibition activity of novel pyrano [2, 3-d] pyrimidine derivatives. Methods: A series of new …

Drug candidates for the treatment of Alzheimer's disease: New findings from 2021 and 2022

SL Motebennur, BP Nandeshwarappa… - Drugs and Drug …, 2023 - mdpi.com
Alzheimer's disease (AD), an ongoing neurodegenerative disorder among the elderly, is
signalized by amnesia, progressive deficiency in cognitive roles, and behavioral deformity …

[HTML][HTML] Butyrylcholinesterase inhibitory activity of peptides identified from yellow field pea (Pisum sativum) enzymatic protein hydrolysates

ND Asen, OD Okagu, CC Udenigwe… - Journal of Functional …, 2023 - Elsevier
Butyrylcholinesterase (BuChE) is an enzyme implicated in Alzheimer's disease due to the
excessive breakdown of neurotransmitters. The study screened and synthesized de novo …

Investigation of spirooxindole-pyrrolidine derivatives as acetylcholinesterase inhibitors using molecular docking/dynamics simulations, bioisosteric replacement, MEP …

R Kherachi, I Daoud, N Melkemi, S Kenouche, M Mettai… - Biologia, 2023 - Springer
Acetylcholinesterase is used as a key target in the treatment of Alzheimer's disease.
Recently, a series of new spirooxindolepyrrolidine derivatives were synthesized and …

Design, synthesis and evaluation of benzo [cd] indol-2 (1H)-one-donepezil hybrids as cholinesterase inhibitors and living cell imaging agents

J Wang, H Zhou, Y Li, Y Mu, J Li, C Hong… - Journal of Molecular …, 2023 - Elsevier
A novel series of benzo [cd] indol-2 (1H)-one-donepezil (BIO-DPZ) hybrids (5a-m, 6a-k) was
designed, synthesized and evaluated as cholinesterase inhibitors and living cell imaging …

Design, synthesis, molecular docking and biological evaluation of β-carboline derivatives as cholinesterase inhibitors

P Baréa, DA dos Santos Yamazaki… - Journal of Molecular …, 2023 - Elsevier
A set of novel β-carboline derivatives were designed and subjected to virtual screening
studies by molecular docking in AChE. Among the compounds investigated, derivatives 1a …