Synthesis and activity studies of analogues of the rat selective toxicant norbormide

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• 作者：David Rennison ; Sergio Bova ; Maurizio Cavalli ; Fern ; a Ricchelli ; Aless ; ra Zulian ; Brian Hopkins ; Margaret A. Brimble
• 关键词：Norbormide ; Rodenticide ; Rat toxicant
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2007
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：15 April 2007
• 卷：15
• 期：8
• 页码：2963-2974
• 文件大小：255 K

摘要

Norbormide [5-(α-hydroxy-α-2-pyridylbenzyl)-7-(α-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.