Identification of 4-aminoquinoline core for the design of new cholinesterase inhibitors
Inhibition of acetylcholinesterase (AChE) using small molecules is still one of the most successful therapeutic strategies in the treatment of Alzheimer’s disease (AD). Previously we reported compound T5369186 with a core of quinolone as a new cholinesterase inhibitor. In the present study, in order...
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doaj-adbcea2f012041718ae1df3d15d323722020-11-24T22:51:21ZengPeerJ Inc.PeerJ2167-83592016-07-014e214010.7717/peerj.2140Identification of 4-aminoquinoline core for the design of new cholinesterase inhibitorsYao Chen0Yaoyao Bian1Yuan Sun2Chen Kang3Sheng Yu4Tingming Fu5Wei Li6Yuqiong Pei7Haopeng Sun8School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, ChinaSchool of Nursing, Nanjing University of Chinese Medicine, Nanjing, ChinaDepartment of Chemistry and Biochemistry, Ohio State University, Columbus, OH, United StatesDivision of Pharmacology, College of Pharmacy, Ohio State University, Columbus, OH, United StatesSchool of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, ChinaSchool of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, ChinaSchool of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, ChinaSchool of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, ChinaDepartment of Medicinal Chemistry, China Pharmaceutical University, Nanjing, ChinaInhibition of acetylcholinesterase (AChE) using small molecules is still one of the most successful therapeutic strategies in the treatment of Alzheimer’s disease (AD). Previously we reported compound T5369186 with a core of quinolone as a new cholinesterase inhibitor. In the present study, in order to identify new cores for the designing of AChE inhibitors, we screened different derivatives of this core with the aim to identify the best core as the starting point for further optimization. Based on the results, we confirmed that only 4-aminoquinoline (compound 04 and 07) had cholinesterase inhibitory effects. Considering the simple structure and high inhibitory potency against AChE, 4-aminoquinoline provides a good starting core for further designing novel multifunctional AChEIs.https://peerj.com/articles/2140.pdfAChEIsInhibitor design4-aminoquinoline core |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Yao Chen Yaoyao Bian Yuan Sun Chen Kang Sheng Yu Tingming Fu Wei Li Yuqiong Pei Haopeng Sun |
spellingShingle |
Yao Chen Yaoyao Bian Yuan Sun Chen Kang Sheng Yu Tingming Fu Wei Li Yuqiong Pei Haopeng Sun Identification of 4-aminoquinoline core for the design of new cholinesterase inhibitors PeerJ AChEIs Inhibitor design 4-aminoquinoline core |
author_facet |
Yao Chen Yaoyao Bian Yuan Sun Chen Kang Sheng Yu Tingming Fu Wei Li Yuqiong Pei Haopeng Sun |
author_sort |
Yao Chen |
title |
Identification of 4-aminoquinoline core for the design of new cholinesterase inhibitors |
title_short |
Identification of 4-aminoquinoline core for the design of new cholinesterase inhibitors |
title_full |
Identification of 4-aminoquinoline core for the design of new cholinesterase inhibitors |
title_fullStr |
Identification of 4-aminoquinoline core for the design of new cholinesterase inhibitors |
title_full_unstemmed |
Identification of 4-aminoquinoline core for the design of new cholinesterase inhibitors |
title_sort |
identification of 4-aminoquinoline core for the design of new cholinesterase inhibitors |
publisher |
PeerJ Inc. |
series |
PeerJ |
issn |
2167-8359 |
publishDate |
2016-07-01 |
description |
Inhibition of acetylcholinesterase (AChE) using small molecules is still one of the most successful therapeutic strategies in the treatment of Alzheimer’s disease (AD). Previously we reported compound T5369186 with a core of quinolone as a new cholinesterase inhibitor. In the present study, in order to identify new cores for the designing of AChE inhibitors, we screened different derivatives of this core with the aim to identify the best core as the starting point for further optimization. Based on the results, we confirmed that only 4-aminoquinoline (compound 04 and 07) had cholinesterase inhibitory effects. Considering the simple structure and high inhibitory potency against AChE, 4-aminoquinoline provides a good starting core for further designing novel multifunctional AChEIs. |
topic |
AChEIs Inhibitor design 4-aminoquinoline core |
url |
https://peerj.com/articles/2140.pdf |
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