- Synthesis and activity studies of analogues of the rat selective toxicant norbormide.
Synthesis and activity studies of analogues of the rat selective toxicant norbormide.
Bioorganic & medicinal chemistry (2007-02-27)
David Rennison, Sergio Bova, Maurizio Cavalli, Fernanda Ricchelli, Alessandra Zulian, Brian Hopkins, Margaret A Brimble
PMID17321141
ABSTRAKT
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.
MATERIAŁY