Synthesis and activity studies of analogues of the rat selective toxicant norbormide
| Autor: | Fernanda Ricchelli, Alessandra Zulian, Brian Hopkins, David Rennison, Margaret A. Brimble, Sergio Bova, Maurizio Cavalli |
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| Rok vydání: | 2007 |
| Předmět: |
Male
Models Molecular synthesis Vasodilator Agents Clinical Biochemistry Molecular Conformation Pharmaceutical Science Mitochondria Liver Vasodilation In Vitro Techniques Mitochondrion Biochemistry Muscle Smooth Vascular Permeability Norbormide Potassium Chloride chemistry.chemical_compound In vivo Drug Discovery Animals Rats Wistar Molecular Biology Cardiotoxicity Chemistry Organic Chemistry Rodenticides Heart Stereoisomerism Biological activity Coronary Vessels Norbornanes rat-specific toxicant In vitro Rats norbormide Molecular Medicine Indicators and Reagents Spectrophotometry Ultraviolet Chromatography Thin Layer norbormide analogues Muscle Contraction Toxicant |
| Zdroj: | Bioorganic & medicinal chemistry 15 (2007): 2963–2974. doi:10.1016/j.bmc.2007.02.012 info:cnr-pdr/source/autori:Rennison D; Bova S; Cavalli M; Ricchelli F; Zulian A; Hopkins B; Brimble MA/titolo:Synthesis and activity studies of analogues of the rat selective toxicant norbormide/doi:10.1016%2Fj.bmc.2007.02.012/rivista:Bioorganic & medicinal chemistry (Print)/anno:2007/pagina_da:2963/pagina_a:2974/intervallo_pagine:2963–2974/volume:15 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2007.02.012 |
| Popis: | Norbormide [5-(alpha-hydroxy-alpha-2-pyridylbenzyl)-7-(alpha-2-pyridylbenzylidene)-5-norbornene-2,3-dicarboximide] (NRB, 1), an existing but infrequently used rodenticide, is known to be uniquely toxic to rats but relatively harmless to other rodents and mammals. A series of NRB-related analogues were prepared to investigate the structural features responsible for, and the in vitro biological markers indicative of, in vivo lethality of the parent molecule in rats. Their synthesis and biological evaluation (vasoconstriction, vasodilation, mitochondrial dysfunction, cardiotoxicity and lethality) is described. |
| Databáze: | OpenAIRE |
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