Novel small molecule therapeutic agents for Alzheimer disease: Focusing on BACE1 and multi-target directed ligands

A Iraji, M Khoshneviszadeh, O Firuzi… - Bioorganic …, 2020 - Elsevier
Alzheimer's Disease (AD) is a progressive neurodegenerative disorder that effects 50 million
people worldwide. In this review, AD pathology and the development of novel therapeutic …

BACE-1 inhibitors: from recent single-target molecules to multitarget compounds for Alzheimer's disease: miniperspective

F Prati, G Bottegoni, ML Bolognesi… - Journal of medicinal …, 2018 - ACS Publications
The amyloid hypothesis has long been the central dogma in drug discovery for Alzheimer's
disease (AD), leading to many small-molecule and biological drug candidates. One major …

Function and toxicity of amyloid beta and recent therapeutic interventions targeting amyloid beta in Alzheimer's disease

K Rajasekhar, M Chakrabarti… - Chemical …, 2015 - pubs.rsc.org
Amyloidogenesis has been implicated in a broad spectrum of diseases in which amyloid
protein is invariably misfolded and deposited in cells and organs. Alzheimer's disease is one …

Synthesis and in-silico studies of some new thiazole carboxamide derivatives with theoretical investigation

N A. Kheder, H Ather, D R. Emam… - Polycyclic Aromatic …, 2024 - Taylor & Francis
Based on the tremendous pharmacological activities of compounds containing thiazole and
carboxamide moieties, the current study aims to prepare new series of thiazole, pyrazole …

Screening Techniques for Drug Discovery in Alzheimer's Disease

S Maniam, S Maniam - ACS omega, 2024 - ACS Publications
Alzheimer's disease (AD) is a neurodegenerative disorder characterized by progressive and
irreversible impairment of memory and other cognitive functions of the aging brain …

Per-residue energy footprints-based pharmacophore modeling as an enhanced in silico approach in drug discovery: a case study on the identification of novel β …

HM Kumalo, ME Soliman - Cellular and Molecular Bioengineering, 2016 - Springer
A further refinement to our previously published “target-bound pharmacophore modeling
approach” is reported herein. Instead of relying on “random” pharmacophores—which is the …

Design, synthesis and biological evaluation of tyrosinase-targeting PROTACs

D Fu, Y Yuan, F Qin, Y Xu, X Cui, G Li, S Yao… - European Journal of …, 2021 - Elsevier
The human tyrosinase is the most prominent therapeutic target for pigmentary skin
disorders. However, the overwhelming majority efforts have been devoted to search …

Fused 1, 4‐Dihydropyridines and Their Corresponding Pyridines: Synthesis, Molecular Modeling and Cholinesterase Inhibition

Z Najafi, M Alaei, A Bahmani, T Akbarzadeh… - …, 2023 - Wiley Online Library
Abstract Novel series of fused 1, 4‐dihydropyridine derivatives were designed and
synthesized. Oxidized to the corresponding pyridines were these dihydropyridines. Both …

Novel 5-oxo-hexahydroquinoline derivatives: design, synthesis, in vitro P-glycoprotein-mediated multidrug resistance reversal profile and molecular dynamics …

O Shahraki, N Edraki, M Khoshneviszadeh… - Drug design …, 2017 - Taylor & Francis
Overexpression of the efflux pump P-glycoprotein (P-gp) is one of the important mechanisms
of multidrug resistance (MDR) in many tumor cells. In this study, 26 novel 5-oxo …

N‐(2‐(Piperazin‐1‐yl)phenyl)arylamide Derivatives as β‐Secretase (BACE1) Inhibitors: Simple Synthesis by Ugi Four‐Component Reaction and Biological …

N Edraki, O Firuzi, Y Fatahi, M Mahdavi… - Archiv der …, 2015 - Wiley Online Library
A novel series of N‐(2‐(piperazin‐1‐yl) phenyl) aryl carboxamide derivatives were simply
synthesized by Ugi‐multicomponent reaction as β‐secretase (BACE1) inhibitors. The …