Structure− brain exposure relationships

SA Hitchcock, LD Pennington - Journal of medicinal chemistry, 2006 - ACS Publications
Healthy functioning of the human brain relies on effective shielding of the sensitive neural
microenvironment from potentially disruptive xenobiotic agents circulating in the periphery …

Molecular mechanisms for Alzheimer's disease: implications for neuroimaging and therapeutics

CL Masters, R Cappai, KJ Barnham… - Journal of …, 2006 - Wiley Online Library
Alzheimer's disease is a progressive neurodegenerative disorder characterised by the
gradual onset of dementia. The pathological hallmarks of the disease are β‐amyloid (Aβ) …

The role and therapeutic targeting of α-, β-and γ-secretase in Alzheimer's disease

R MacLeod, EK Hillert, RT Cameron… - Future science OA, 2015 - Taylor & Francis
Alzheimer's disease (AD) is the most common form of dementia in the elderly and its
prevalence is set to increase rapidly in coming decades. However, there are as yet no …

Alzheimer's centennial legacy: prospects for rational therapeutic intervention targeting the Aβ amyloid pathway

CL Masters, K Beyreuther - Brain, 2006 - academic.oup.com
It is now 100 years since the nosological definition of Alzheimer's disease emerged. In the
first 80 years, very little progress was made in understanding the mechanisms that caused …

Recent progress in the medicinal chemistry of γ-secretase inhibitors

RE Olson, CF Albright - Current topics in medicinal chemistry, 2008 - ingentaconnect.com
Aβ is implicated in the initiation and progression of Alzheimer's disease (AD) by the
phenotypic analysis of mutations in three human genes that lead to inherited, early forms of …

Novel acetamidothiazole derivatives: synthesis and in vitro anticancer evaluation

AR Ali, ER El-Bendary, MA Ghaly, IA Shehata - European Journal of …, 2013 - Elsevier
A novel series of acetamide derivatives possessing both 2-imino-4-arylthiazoles and
morpholine or different piperazines were synthesized and characterized by IR, 1 H NMR, 13 …

Inhibitors and modulators of β-and γ-secretase

B Schmidt, S Baumann, HA Braun… - Current Topics in …, 2006 - ingentaconnect.com
Most gene mutations associated with Alzheimer's disease point to the metabolism of amyloid
precursor protein as potential cause. The β-and γ-secretases are two executioners of …

Synthesis and anticancer activities of some thiazole derivatives

I Kayagil, S Demirayak - Phosphorus, Sulfur, and Silicon, 2009 - Taylor & Francis
In this study, 2-substituted 4-[3/4-(4-arylthiazole-2-yl) aminophenyl] thiazole derivatives and
2-[4-[2-substituted 4-methylthiazole-5-yl] thiazole-2-yl] amino-5-arylidenethiazoline-4-one …

Use of gamma secretase inhibitors and notch pathway inhibitors for treatment and prevention of renal disease

K Susztak, B Bielesz, TG Niranjan - US Patent 8,377,886, 2013 - Google Patents
(*) Notice: Subject to any disclaimer, the term of this W000-b.* liprevent).* patent is extended
or adjusted under 35 Vanes et al. in Nature 435 (16), pp. 959-963 (2005).* USC 154 (b) by …

Enhanced delivery of γ-secretase inhibitor DAPT into the brain via an ascorbic acid mediated strategy

G Quéléver, P Kachidian, C Melon, C Garino… - Organic & …, 2005 - pubs.rsc.org
Inhibition of γ-secretase, one of the enzymes responsible for the cleavage of the amyloid
precursor protein (APP) to produce pathogenic Aβ peptides, is an attractive approach for the …