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Hybrids of oxoisoaporphine-tacrine congeners: novel acetylcholinesterase and acetylcholinesterase-induced β-amyloid aggregation inhibitors.
Eur J Med Chem. 2011 Oct; 46(10):4970-9.EJ

Abstract

A series of dual binding site acetylcholinesterase (AChE) inhibitors have been designed, synthesized, and tested for their ability to inhibit AChE, butyrylcholinesterase (BChE), AChE-induced and self-induced β-amyloid (Aβ) aggregation. The new hybrids consist of a unit of 1-azabenzanthrone and a tacrine or its congener, connected through an oligomethylene linker containing an amine group at variable position. These hybrids exhibit high AChE inhibitory activity with IC(50) values in the nanomolar range in most cases. Moreover, five out of the 12 hybrids of this series, particularly those bearing a tetrahydroacridine moiety, exhibit a significant in vitro inhibitory activity toward the AChE-induced and self-induced Aβ aggregation, which makes them promising anti-Alzheimer drug candidates.

Authors+Show Affiliations

State Key Laboratory Cultivation Base for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry & Chemical Engineering of Guangxi Normal University, Guilin 541004, PR China.No affiliation info availableNo 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

21871694

Citation

Tang, Huang, et al. "Hybrids of Oxoisoaporphine-tacrine Congeners: Novel Acetylcholinesterase and Acetylcholinesterase-induced Β-amyloid Aggregation Inhibitors." European Journal of Medicinal Chemistry, vol. 46, no. 10, 2011, pp. 4970-9.
Tang H, Zhao LZ, Zhao HT, et al. Hybrids of oxoisoaporphine-tacrine congeners: novel acetylcholinesterase and acetylcholinesterase-induced β-amyloid aggregation inhibitors. Eur J Med Chem. 2011;46(10):4970-9.
Tang, H., Zhao, L. Z., Zhao, H. T., Huang, S. L., Zhong, S. M., Qin, J. K., Chen, Z. F., Huang, Z. S., & Liang, H. (2011). Hybrids of oxoisoaporphine-tacrine congeners: novel acetylcholinesterase and acetylcholinesterase-induced β-amyloid aggregation inhibitors. European Journal of Medicinal Chemistry, 46(10), 4970-9. https://doi.org/10.1016/j.ejmech.2011.08.002
Tang H, et al. Hybrids of Oxoisoaporphine-tacrine Congeners: Novel Acetylcholinesterase and Acetylcholinesterase-induced Β-amyloid Aggregation Inhibitors. Eur J Med Chem. 2011;46(10):4970-9. PubMed PMID: 21871694.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Hybrids of oxoisoaporphine-tacrine congeners: novel acetylcholinesterase and acetylcholinesterase-induced β-amyloid aggregation inhibitors. AU - Tang,Huang, AU - Zhao,Li-Zhen, AU - Zhao,Hao-Tao, AU - Huang,Shi-Liang, AU - Zhong,Shu-Ming, AU - Qin,Jiang-Ke, AU - Chen,Zhen-Feng, AU - Huang,Zhi-Shu, AU - Liang,Hong, Y1 - 2011/08/07/ PY - 2011/04/05/received PY - 2011/07/12/revised PY - 2011/08/01/accepted PY - 2011/8/30/entrez PY - 2011/8/30/pubmed PY - 2012/2/18/medline SP - 4970 EP - 9 JF - European journal of medicinal chemistry JO - Eur J Med Chem VL - 46 IS - 10 N2 - A series of dual binding site acetylcholinesterase (AChE) inhibitors have been designed, synthesized, and tested for their ability to inhibit AChE, butyrylcholinesterase (BChE), AChE-induced and self-induced β-amyloid (Aβ) aggregation. The new hybrids consist of a unit of 1-azabenzanthrone and a tacrine or its congener, connected through an oligomethylene linker containing an amine group at variable position. These hybrids exhibit high AChE inhibitory activity with IC(50) values in the nanomolar range in most cases. Moreover, five out of the 12 hybrids of this series, particularly those bearing a tetrahydroacridine moiety, exhibit a significant in vitro inhibitory activity toward the AChE-induced and self-induced Aβ aggregation, which makes them promising anti-Alzheimer drug candidates. SN - 1768-3254 UR - https://www.unboundmedicine.com/medline/citation/21871694/Hybrids_of_oxoisoaporphine_tacrine_congeners:_novel_acetylcholinesterase_and_acetylcholinesterase_induced_β_amyloid_aggregation_inhibitors_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(11)00574-5 DB - PRIME DP - Unbound Medicine ER -