Structure-activity relationships in platelet-activating factor (PAF). 8. Tetrahydrofuran derivatives as dual PAF antagonists and acetylcholinesterase inhibitors: anti-acetylcholinesterase activity and comparative SAR
| Autor: | Laurence Le Texier, Edith Favre, Nello Ronzani, France Massicot, Nadine Blavet, Edouardo Pirotzky, Jean-Jacques Godfroid |
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| Rok vydání: | 1996 |
| Předmět: |
Adult
Male Aché Immunology chemistry.chemical_compound Mice Structure-Activity Relationship In vivo Structure–activity relationship Animals Humans Platelet Activating Factor Furans Tetrahydrofuran Pharmacology Platelet-activating factor Acetylcholinesterase language.human_language In vitro Mice Inbred C57BL chemistry Biochemistry Toxicity language Cholinesterase Inhibitors |
| Zdroj: | Journal of lipid mediators and cell signalling. 13(3) |
| ISSN: | 0929-7855 |
| Popis: | 2,5-disubstituted tetrahydrofuran derivatives display a dual functionality: they are PAF antagonists and acetylcholinesterase (AChE) inhibitors. In vitro anti-AChE activity and in vivo trials are presented herein. These compounds are competitive and potent AChE inhibitors. Structure-activity relationships are described and compared with PAF-antagonist results. The presence of an onium group, a suitable distance supplied by a chain of 7 or 10 carbon atoms separating the function from the polar head and an appreciable chain hydrophobicity (4sigma f7) are the main features required for a dual activity. The derivatives are evaluated in a mouse passive avoidance model. Only compounds with both activities are able to reverse scopolamine-induced amnesia. In addition, they display a very weak toxicity. |
| Databáze: | OpenAIRE |
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