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Structure-activity relationships in platelet-activating factor (PAF). 8. Tetrahydrofuran derivatives as dual PAF antagonists and acetylcholinesterase inhibitors: anti-acetylcholinesterase activity and comparative SAR

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 relatio... Full description

Journal Title: Journal of Lipid Mediators and Cell Signalling 1996, Vol.13(3), pp.207-222
Main Author: Texier, Laurence Le
Other Authors: Favre, Edith , Ronzani, Nello , Massicot, France , Blavet, Nadine , Pirotzky, Edouardo , Godfroid, Jean-Jacques
Format: Electronic Article Electronic Article
Language: English
Subjects:
ID: ISSN: 0929-7855 ; DOI: 10.1016/0929-7855(95)00053-4
Link: https://www.sciencedirect.com/science/article/pii/0929785595000534
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recordid: elsevier_sdoi_10_1016_0929_7855_95_00053_4
title: Structure-activity relationships in platelet-activating factor (PAF). 8. Tetrahydrofuran derivatives as dual PAF antagonists and acetylcholinesterase inhibitors: anti-acetylcholinesterase activity and comparative SAR
format: Article
creator:
  • Texier, Laurence Le
  • Favre, Edith
  • Ronzani, Nello
  • Massicot, France
  • Blavet, Nadine
  • Pirotzky, Edouardo
  • Godfroid, Jean-Jacques
subjects:
  • Tetrahydrofuran
  • Acytetylcholinesterase Inhibitor
  • PAF Antagonist
  • Structure-Activity Relationship
  • Alzheimer'S Disease
  • Anatomy & Physiology
ispartof: Journal of Lipid Mediators and Cell Signalling, 1996, Vol.13(3), pp.207-222
description: 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 (4 < sigma f < 7) 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.
language: eng
source:
identifier: ISSN: 0929-7855 ; DOI: 10.1016/0929-7855(95)00053-4
fulltext: fulltext
issn:
  • 0929-7855
  • 09297855
url: Link


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titleStructure-activity relationships in platelet-activating factor (PAF). 8. Tetrahydrofuran derivatives as dual PAF antagonists and acetylcholinesterase inhibitors: anti-acetylcholinesterase activity and comparative SAR
creatorTexier, Laurence Le ; Favre, Edith ; Ronzani, Nello ; Massicot, France ; Blavet, Nadine ; Pirotzky, Edouardo ; Godfroid, Jean-Jacques
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identifierISSN: 0929-7855 ; DOI: 10.1016/0929-7855(95)00053-4
subjectTetrahydrofuran ; Acytetylcholinesterase Inhibitor ; PAF Antagonist ; Structure-Activity Relationship ; Alzheimer'S Disease ; Anatomy & Physiology
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description2,5-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 (4 < sigma f < 7) 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.
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