Abstract:
:The synthesis of tacrine-thiadiazolidinone hybrids is described. These compounds are designed as dual acetylcholinesterase inhibitors binding simultaneously to the peripheral and catalytic sites of the enzyme. All tested compounds exhibit significant AChE inhibitory activity. Competition assays using propidium as reference of selective ligand for the peripheral anionic site on acetylcholinesterase indicates the influence of the designed compounds over the peripheral site. They can be considered as new leads in the optimization of Alzheimer's disease modifying agents.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Dorronsoro I,Alonso D,Castro A,del Monte M,García-Palomero E,Martínez Adoi
10.1002/ardp.200400919keywords:
subject
Has Abstractpub_date
2005-01-01 00:00:00pages
18-23issue
1eissn
0365-6233issn
1521-4184journal_volume
338pub_type
杂志文章abstract::MXT-M-3,2 breast cancer implanted into female B6D2F1 mice accelerates the growth of an identical second tumor. This process is accompanied by a significant increase of the granulocyte and monocyte numbers in the blood and of the granulocyte and macrophage numbers in the spleen. A significant positive correlation of st...
journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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更新日期:2008-06-01 00:00:00
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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pub_type: 杂志文章
doi:10.1002/ardp.19953280903
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abstract::Gypsogenin (1) was obtained by acidic hydrolysis from its saponin. While the parent compound 1 acted as a selective inhibitor for butyrylcholinesterase (from equus) possessing a moderate mixed-type inhibition of the enzyme, Ki values as low as 2.67 ± 0.59 μM were determined for (3β,4α) 3-O-acetyl-olean-12-ene-23,28-di...
journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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