Novel Benzothiazole-Based Ureas as 17 beta-HSD10 Inhibitors, A Potential Alzheimer's Disease Treatment
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62690094%3A18470%2F19%3A50015709" target="_blank" >RIV/62690094:18470/19:50015709 - isvavai.cz</a>
Alternative codes found
RIV/00179906:_____/19:10398712
Result on the web
<a href="https://www.mdpi.com/1420-3049/24/15/2757" target="_blank" >https://www.mdpi.com/1420-3049/24/15/2757</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/molecules24152757" target="_blank" >10.3390/molecules24152757</a>
Alternative languages
Result language
angličtina
Original language name
Novel Benzothiazole-Based Ureas as 17 beta-HSD10 Inhibitors, A Potential Alzheimer's Disease Treatment
Original language description
It has long been established that mitochondrial dysfunction in Alzheimer's disease (AD) patients can trigger pathological changes in cell metabolism by altering metabolic enzymes such as the mitochondrial 17 beta-hydroxysteroid dehydrogenase type 10 (17 beta-HSD10), also known as amyloid-binding alcohol dehydrogenase (ABAD). We and others have shown that frentizole and riluzole derivatives can inhibit 17 beta-HSD10 and that this inhibition is beneficial and holds therapeutic merit for the treatment of AD. Here we evaluate several novel series based on benzothiazolylurea scaffold evaluating key structural and activity relationships required for the inhibition of 17 beta-HSD10. Results show that the most promising of these compounds have markedly increased potency on our previously published inhibitors, with the most promising exhibiting advantageous features like low cytotoxicity and target engagement in living cells.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30107 - Medicinal chemistry
Result continuities
Project
<a href="/en/project/EF18_069%2F0010054" target="_blank" >EF18_069/0010054: IT4Neuro(degeneration)</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2019
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Molecules
ISSN
1420-3049
e-ISSN
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Volume of the periodical
24
Issue of the periodical within the volume
15
Country of publishing house
CH - SWITZERLAND
Number of pages
23
Pages from-to
"Article Number: 2757"
UT code for WoS article
000482441100080
EID of the result in the Scopus database
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