title: 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.
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, China; Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Nanjing University of Chinese Medicine, Nanjing, China.
authors.forename: Yao
authors.initials: Y
authors.lastname: Chen
authors.affiliation: School of Nursing, Nanjing University of Chinese Medicine , Nanjing , China.
authors.forename: Yaoyao
authors.initials: Y
authors.lastname: Bian
authors.affiliation: Department of Chemistry and Biochemistry, Ohio State University , Columbus , OH , United States.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Sun
authors.affiliation: Division of Pharmacology, College of Pharmacy, Ohio State University , Columbus , OH , United States.
authors.forename: Chen
authors.initials: C
authors.lastname: Kang
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine , Nanjing , China.
authors.forename: Sheng
authors.initials: S
authors.lastname: Yu
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, China; Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Nanjing University of Chinese Medicine, Nanjing, China.
authors.forename: Tingming
authors.initials: T
authors.lastname: Fu
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine , Nanjing , China.
authors.forename: Wei
authors.initials: W
authors.lastname: Li
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine , Nanjing , China.
authors.forename: Yuqiong
authors.initials: Y
authors.lastname: Pei
authors.affiliation: Department of Medicinal Chemistry, China Pharmaceutical University , Nanjing , China.
authors.forename: Haopeng
authors.initials: H
authors.lastname: Sun
keywords: 4-aminoquinoline core; AChEIs; Inhibitor design