Contemporary synthetic strategies in organofluorine chemistry

R Britton, V Gouverneur, JH Lin, M Meanwell… - Nature Reviews …, 2021 - nature.com
Fluorinated molecules have a wide range of applications and are used as medicines,
agrochemicals and refrigerants and in smartphone liquid crystal displays, photovoltaic solar …

Targeting amyloidogenic processing of APP in Alzheimer's disease

J Zhao, X Liu, W Xia, Y Zhang, C Wang - Frontiers in molecular …, 2020 - frontiersin.org
Alzheimer's disease (AD) is the most common type of senile dementia, characterized by
neurofibrillary tangle and amyloid plaque in brain pathology. Major efforts in AD drug were …

Bace1 inhibitors for Alzheimer's disease: the past, present and any future?

FH Bazzari, AH Bazzari - Molecules, 2022 - mdpi.com
Alzheimer's disease (AD) is the most prevalent neurodegenerative disorder and the most
common cause of dementia in the elderly. The complexity of AD has hindered the …

An analysis of successful hit-to-clinical candidate pairs

DG Brown - Journal of medicinal chemistry, 2023 - ACS Publications
An analysis of 156 published clinical candidates from the Journal of Medicinal Chemistry
between 2018 and 2021 was conducted to identify lead generation strategies most …

Recent advances of thiazole hybrids in biological applications

M Gümüş, M Yakan, İ Koca - Future Medicinal Chemistry, 2019 - Taylor & Francis
Thiazoles have attracted much synthetic interest due to their wide variety of biological
properties and are important members of heterocyclic compounds. In recent years, studies …

Selective secretase targeting for Alzheimer's disease therapy

A Miranda, E Montiel, H Ulrich… - Journal of Alzheimer's …, 2021 - content.iospress.com
Alzheimer's disease (AD) is associated with marked atrophy of the cerebral cortex and
accumulation of amyloid plaques and neurofibrillary tangles. Amyloid plaques are formed by …

New evolutions in the BACE1 inhibitor field from 2014 to 2018

CC Hsiao, F Rombouts, HJM Gijsen - Bioorganic & medicinal chemistry …, 2019 - Elsevier
Abstract β-Site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors offer the
potential of disease-modifying treatment for Alzheimer's disease (AD). Since 2014, major …

BACE1 inhibitors for Alzheimer's Disease: current challenges and Future perspectives

JRM Coimbra, R Resende… - Journal of …, 2024 - journals.sagepub.com
Disease-modifying therapies (DMT) for Alzheimer's disease (AD) are highly longed-for. In
this quest, anti-amyloid therapies take center stage supported by genetic facts that highlight …

Discovery of Umibecestat (CNP520): A potent, selective, and efficacious β-secretase (BACE1) inhibitor for the prevention of Alzheimer's disease

R Machauer, R Lueoend, K Hurth… - Journal of medicinal …, 2021 - ACS Publications
After identification of lead compound 6, 5-amino-1, 4-oxazine BACE1 inhibitors were
optimized in order to improve potency, brain penetration, and metabolic stability. Insertion of …

Secretase promotes AD progression: simultaneously cleave Notch and APP

KF Yang, JY Zhang, M Feng, K Yao, YY Liu… - Frontiers in Aging …, 2024 - frontiersin.org
Alzheimer's disease (AD) involves complex pathological mechanisms. Secretases include
membrane protein extracellular structural domain proteases and intramembrane proteases …