Highlights in BACE1 inhibitors for Alzheimer's disease treatment

JRM Coimbra, DFF Marques, SJ Baptista… - Frontiers in …, 2018 - frontiersin.org
Alzheimer's disease (AD) is a severe neurodegenerative disorder and the most common
type of dementia in the elderly. The clinical symptoms of AD include a progressive loss of …

Guanidine-based β amyloid precursor protein cleavage enzyme 1 (BACE-1) inhibitors for the Alzheimer's disease (AD): a review

P Gehlot, S Kumar, VK Vyas, BS Choudhary… - Bioorganic & Medicinal …, 2022 - Elsevier
Alzheimer's disease (AD) is an irreversible, progressive neurological disorder characterized
by amyloid plaques, hyperphosphorylated tau protein (hyper p-tau), neuronal damage …

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 …

The chemistry and biology of guanidine natural products

RGS Berlinck, AF Bertonha, M Takaki… - Natural product …, 2017 - pubs.rsc.org
Covering: 2015 and 2016 The chemistry and biology of natural guanidines isolated from
microbial culture media, from marine invertebrates, as well as from terrestrial plants and …

Unveiling the potential of novel indol-3-yl-phenyl allylidene hydrazine carboximidamide derivatives as AChE/BACE 1 dual inhibitors: a combined in silico, synthesis …

A Sharma, S Rudrawar, A Sharma, SB Bharate… - RSC …, 2024 - pubs.rsc.org
Considering the failure of many enzyme inhibitors for Alzheimer's disease (AD), research is
now focused on multi-target directed drug discovery. In this paper, inhibition of two essential …

Design, synthesis, in silico, and in vitro evaluation of pyrrol-2-yl-phenyl allylidene hydrazine carboximidamide derivatives as AChE/BACE 1 dual inhibitors

A Sharma, S Rudrawar, A Sharma, SB Bharate… - RSC …, 2024 - pubs.rsc.org
Alzheimer's disease (AD) manifests as a progressive decline in cognitive function and
mental behavior. Targeting two crucial enzymes associated with AD, acetylcholinesterase …

DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's …

X Qiang, Y Li, X Yang, L Luo, R Xu, Y Zheng… - Bioorganic & Medicinal …, 2017 - Elsevier
Considering the complex etiology of Alzheimer's disease (AD), multifunctional agents may
be beneficial for the treatment of this disease. A series of DL-3-n-butylphthalide-Edaravone …

Electroacupuncture mitigates hippocampal cognitive impairments by reducing BACE1 deposition and activating PKA in APP/PS1 double transgenic mice

Y Tang, S Shao, Y Guo, Y Zhou, J Cao, A Xu… - Neural …, 2019 - Wiley Online Library
Increased amyloid‐β (Aβ) plaque deposition is thought to be the main cause of Alzheimer's
disease (AD). β‐Site amyloid precursor protein cleaving enzyme 1 (BACE1) is the key …

Design, synthesis, evaluation and molecular modeling study of 4-N-phenylaminoquinolines for Alzheimer disease treatment

J Zhu, LN Wang, R Cai, SQ Geng, YF Dong… - Bioorganic & Medicinal …, 2019 - Elsevier
Dual binding site acetylcholinesterase (AChE) inhibitors and butyrylcholinesterase (BChE)
inhibitors have recently emerged as two classes of new anti-Alzheimer agents to positively …

2-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl) acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies

G Yan, L Hao, Y Niu, W Huang, W Wang, F Xu… - European journal of …, 2017 - Elsevier
In this work, a series of 2-substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)
acetamide derivatives were developed as β-secretase (BACE-1) inhibitors. Supported by …