Modern advances in heterocyclic chemistry in drug discovery

AP Taylor, RP Robinson, YM Fobian… - Organic & …, 2016 - pubs.rsc.org
New advances in synthetic methodologies that allow rapid access to a wide variety of
functionalized heterocyclic compounds are of critical importance to the medicinal chemist as …

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 …

Where does the fluorine come from? A review on the challenges associated with the synthesis of organofluorine compounds

S Caron - Organic Process Research & Development, 2020 - ACS Publications
Fluorinated organic molecules are increasingly being prepared for a variety of applications,
including pharmaceutical products. However, the supply chain to access the necessary raw …

Discovery of the 3-imino-1, 2, 4-thiadiazinane 1, 1-dioxide derivative verubecestat (MK-8931)–a β-site amyloid precursor protein cleaving enzyme 1 inhibitor for the …

JD Scott, SW Li, APJ Brunskill, X Chen, K Cox… - 2016 - ACS Publications
Verubecestat 3 (MK-8931), a diaryl amide-substituted 3-imino-1, 2, 4-thiadiazinane 1, 1-
dioxide derivative, is a high-affinity β-site amyloid precursor protein cleaving enzyme 1 …

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 …

AZD3293: a novel, orally active BACE1 inhibitor with high potency and permeability and markedly slow off-rate kinetics

S Eketjäll, J Janson, K Kaspersson… - Journal of …, 2016 - content.iospress.com
A growing body of pathological, biomarker, genetic, and mechanistic data suggests that
amyloid accumulation, as a result of changes in production, processing, and/or clearance of …

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 …

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 …

Catalytic diastereo-and enantioselective additions of versatile allyl groups to N–H ketimines

H Jang, F Romiti, S Torker, AH Hoveyda - Nature chemistry, 2017 - nature.com
There are many biologically active organic molecules that contain one or more nitrogen-
containing moieties, and broadly applicable and efficient catalytic transformations that …

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 …