Synthesis and activity studies of analogues of the rat selective toxicant norbormide |
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Authors: | Rennison David Bova Sergio Cavalli Maurizio Ricchelli Fernanda Zulian Alessandra Hopkins Brian Brimble Margaret A |
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Affiliation: | Department of Chemistry, University of Auckland, 23 Symonds Street, Auckland, New Zealand. d.rennison@auckland.ac.nz |
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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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