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Synthesis and evaluation of heterobivalent tacrine derivatives as potential multi-functional anti-Alzheimer agents.
Eur J Med Chem. 2011 Jun; 46(6):2609-16.EJ

Abstract

A new series of heterobivalent tacrine derivatives were designed, synthesized and evaluated as potential multi-functional anti-Alzheimer agents for their inhibitory activity on cholinesterases, antioxidant activity and self-induced β-amyloid (Aβ) aggregation. All these synthesized compounds had potent inhibition activity on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) at nanomolar range. A Lineweaver-Burk plot and molecular modeling study showed that these compounds targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. The compounds containing hydroxyl group showed potent peroxyl radical absorbance activity. In addition, compound 5j exhibited higher self-induced Aβ aggregation inhibitory activity than curcumin, which could become a multi-functional agent for further development for the treatment of AD.

Authors+Show Affiliations

School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, People's Republic of China.No 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

21497959

Citation

Luo, Wen, et al. "Synthesis and Evaluation of Heterobivalent Tacrine Derivatives as Potential Multi-functional anti-Alzheimer Agents." European Journal of Medicinal Chemistry, vol. 46, no. 6, 2011, pp. 2609-16.
Luo W, Li YP, He Y, et al. Synthesis and evaluation of heterobivalent tacrine derivatives as potential multi-functional anti-Alzheimer agents. Eur J Med Chem. 2011;46(6):2609-16.
Luo, W., Li, Y. P., He, Y., Huang, S. L., Li, D., Gu, L. Q., & Huang, Z. S. (2011). Synthesis and evaluation of heterobivalent tacrine derivatives as potential multi-functional anti-Alzheimer agents. European Journal of Medicinal Chemistry, 46(6), 2609-16. https://doi.org/10.1016/j.ejmech.2011.03.058
Luo W, et al. Synthesis and Evaluation of Heterobivalent Tacrine Derivatives as Potential Multi-functional anti-Alzheimer Agents. Eur J Med Chem. 2011;46(6):2609-16. PubMed PMID: 21497959.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and evaluation of heterobivalent tacrine derivatives as potential multi-functional anti-Alzheimer agents. AU - Luo,Wen, AU - Li,Yan-Ping, AU - He,Yan, AU - Huang,Shi-Liang, AU - Li,Ding, AU - Gu,Lian-Quan, AU - Huang,Zhi-Shu, Y1 - 2011/04/03/ PY - 2010/12/12/received PY - 2011/02/26/revised PY - 2011/03/25/accepted PY - 2011/4/19/entrez PY - 2011/4/19/pubmed PY - 2011/9/13/medline SP - 2609 EP - 16 JF - European journal of medicinal chemistry JO - Eur J Med Chem VL - 46 IS - 6 N2 - A new series of heterobivalent tacrine derivatives were designed, synthesized and evaluated as potential multi-functional anti-Alzheimer agents for their inhibitory activity on cholinesterases, antioxidant activity and self-induced β-amyloid (Aβ) aggregation. All these synthesized compounds had potent inhibition activity on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) at nanomolar range. A Lineweaver-Burk plot and molecular modeling study showed that these compounds targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. The compounds containing hydroxyl group showed potent peroxyl radical absorbance activity. In addition, compound 5j exhibited higher self-induced Aβ aggregation inhibitory activity than curcumin, which could become a multi-functional agent for further development for the treatment of AD. SN - 1768-3254 UR - https://www.unboundmedicine.com/medline/citation/21497959/Synthesis_and_evaluation_of_heterobivalent_tacrine_derivatives_as_potential_multi_functional_anti_Alzheimer_agents_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(11)00275-3 DB - PRIME DP - Unbound Medicine ER -