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

Bioorganic & Medicinal Chemistry
David RennisonMargaret A Brimble

Abstract

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.

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Citations

May 19, 2007·Biochimica Et Biophysica Acta·Alessandra ZulianFernanda Ricchelli
Aug 27, 2015·Organic Letters·Hailong YangXumu Zhang
Feb 9, 2008·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ellis Benjamin, Yousef Hijji
Jun 13, 2019·Chemical Communications : Chem Comm·Baokun QiaoZhiyong Jiang
Feb 27, 2013·Chemical Communications : Chem Comm·Adam J LoweFrederick M Pfeffer
Jun 10, 2021·Chemistry : a European Journal·Raphael E WildermuthThomas Magauer
Nov 24, 2011·The Journal of Organic Chemistry·Xiaoming TaoZhaoguo Zhang

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