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Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors.
Bioorg Med Chem. 2009 Sep 15; 17(18):6692-8.BM

Abstract

A new series of flavonoid derivatives have been designed, synthesized and evaluated as potent AChE inhibitors. Most of them showed more potent inhibitory activities to AChE than rivastigmine. The most potent inhibitor isoflavone derivative 10d inhibit AChE with a IC(50) of 4 nM and showed high BChE/AChE inhibition ratio (4575-fold), superior to donepezil (IC(50)=12 nM, 389-fold). Molecular docking studies were also performed to explore the detailed interaction with AChE.

Authors+Show Affiliations

ZJU-ENS Joint Laboratory of Medicinal Chemistry, School of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, PR China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

19692250

Citation

Sheng, Rong, et al. "Design, Synthesis and Evaluation of Flavonoid Derivatives as Potent AChE Inhibitors." Bioorganic & Medicinal Chemistry, vol. 17, no. 18, 2009, pp. 6692-8.
Sheng R, Lin X, Zhang J, et al. Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors. Bioorg Med Chem. 2009;17(18):6692-8.
Sheng, R., Lin, X., Zhang, J., Chol, K. S., Huang, W., Yang, B., He, Q., & Hu, Y. (2009). Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors. Bioorganic & Medicinal Chemistry, 17(18), 6692-8. https://doi.org/10.1016/j.bmc.2009.07.072
Sheng R, et al. Design, Synthesis and Evaluation of Flavonoid Derivatives as Potent AChE Inhibitors. Bioorg Med Chem. 2009 Sep 15;17(18):6692-8. PubMed PMID: 19692250.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors. AU - Sheng,Rong, AU - Lin,Xiao, AU - Zhang,Jing, AU - Chol,Kim Sun, AU - Huang,Wenhai, AU - Yang,Bo, AU - He,Qiaojun, AU - Hu,Yongzhou, Y1 - 2009/08/03/ PY - 2009/06/11/received PY - 2009/07/24/revised PY - 2009/07/24/accepted PY - 2009/8/21/entrez PY - 2009/8/21/pubmed PY - 2009/12/18/medline SP - 6692 EP - 8 JF - Bioorganic & medicinal chemistry JO - Bioorg Med Chem VL - 17 IS - 18 N2 - A new series of flavonoid derivatives have been designed, synthesized and evaluated as potent AChE inhibitors. Most of them showed more potent inhibitory activities to AChE than rivastigmine. The most potent inhibitor isoflavone derivative 10d inhibit AChE with a IC(50) of 4 nM and showed high BChE/AChE inhibition ratio (4575-fold), superior to donepezil (IC(50)=12 nM, 389-fold). Molecular docking studies were also performed to explore the detailed interaction with AChE. SN - 1464-3391 UR - https://www.unboundmedicine.com/medline/citation/19692250/Design_synthesis_and_evaluation_of_flavonoid_derivatives_as_potent_AChE_inhibitors_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0968-0896(09)00718-4 DB - PRIME DP - Unbound Medicine ER -