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Identification of 4-aminoquinoline core for the design of new cholinesterase inhibitors.

ABSTRACT: 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.

SUBMITTER: Chen Y

PROVIDER: S-EPMC4941764 | biostudies-literature | 2016

REPOSITORIES: biostudies-literature

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Identification of 4-aminoquinoline core for the design of new cholinesterase inhibitors.

Chen Yao Y Bian Yaoyao Y Sun Yuan Y Kang Chen C Yu Sheng S Fu Tingming T Li Wei W Pei Yuqiong Y Sun Haopeng H

PeerJ 20160707

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 ...[more]

PMID: 27441112

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