Design, synthesis, and biological evaluation of new ALDH2 activators
Joint Authors
Chen, Xin
Tian, Wei
Hu, Jian
Zhou, Ruolan
Zhang, Yuefan
Lv, Jiaguo
Zhu, Ju
Pan, Xianhua
Zheng, Canhui
Source
Journal of Saudi Chemical Society
Issue
Vol. 23, Issue 3 (31 Mar. 2019), pp.255-262, 8 p.
Publisher
Publication Date
2019-03-31
Country of Publication
Saudi Arabia
No. of Pages
8
Main Subjects
Topics
Abstract EN
Mitochondrial aldehyde dehydrogenase 2 (ALDH2) is an important enzyme response for the metabolism or detoxification of toxic aldehydes, in particular acetaldehyde and 4-hydroxynonenal (4-HNE), which were important risk factors for acute alcoholism and stroke respectively.
A special variant ALDH2*2 with reduced enzymatic activity was carried by a high percentage of East Asians, especially Han Chinese, and that could increase the risk of these diseases further.
Therefore, ALDH2 activators had important potential clinical values.
N-benzylbenzamide compounds represented by Alda-1 were the only ALDH2-specific activators that have been reported so far.
In this study, three new classes of compounds were modified from Alda-1 to improve their water-solubility and then drug-like properties.
The results showed that all compounds had increased water solubility and two classes of compounds exhibited good activation activity.
Among them, compound I-6 showed the best activity.
American Psychological Association (APA)
Hu, Jian& Tian, Wei& Zhou, Ruolan& Zhang, Yuefan& Lv, Jiaguo& Zhu, Ju…[et al.]. 2019. Design, synthesis, and biological evaluation of new ALDH2 activators. Journal of Saudi Chemical Society،Vol. 23, no. 3, pp.255-262.
https://search.emarefa.net/detail/BIM-887383
Modern Language Association (MLA)
Hu, Jian…[et al.]. Design, synthesis, and biological evaluation of new ALDH2 activators. Journal of Saudi Chemical Society Vol. 23, no. 3 (Mar. 2019), pp.255-262.
https://search.emarefa.net/detail/BIM-887383
American Medical Association (AMA)
Hu, Jian& Tian, Wei& Zhou, Ruolan& Zhang, Yuefan& Lv, Jiaguo& Zhu, Ju…[et al.]. Design, synthesis, and biological evaluation of new ALDH2 activators. Journal of Saudi Chemical Society. 2019. Vol. 23, no. 3, pp.255-262.
https://search.emarefa.net/detail/BIM-887383
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references : p. 262
Record ID
BIM-887383