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Separation, characterisation and biological evaluation of the individual isomers of the rat selective toxicant norbormide – isolated using a chemical derivatization strategy

Jay-Smith, M, Wang, ZL, Al-Kassas, R, Murphy, EC, Shapiro, L, Eason, CT, Brimble, MA and Rennison, D (2021) Separation, characterisation and biological evaluation of the individual isomers of the rat selective toxicant norbormide – isolated using a chemical derivatization strategy. Arkivoc, 2021 (10). ISSN 1551-7012

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Abstract

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/mammals. However, as an acute vasoactive, NRB has a rapid onset of action, often leading to sub-lethal uptake/bait shyness. Recently, it was brought to our attention that baits containing two independently sourced batches of NRB (which differed noticeably in their stereochemical composition) displayed markedly different palatability/efficacy profiles in rats. Accordingly, with a view to independently evaluating the individual isomers of NRB in rats by means of a palatability and efficacy bait trial, this research describes the isolation of the individual isomers of endo-NRB (Y, V, W and U) from the parent mixture, by means of a chemical derivatization strategy.

Item Type: Article
Uncontrolled Keywords: 0304 Medicinal and Biomolecular Chemistry, 0305 Organic Chemistry
Subjects: Q Science > QD Chemistry
Q Science > QH Natural history > QH301 Biology
Q Science > QR Microbiology
R Medicine > RM Therapeutics. Pharmacology
Divisions: Pharmacy & Biomolecular Sciences
Publisher: ARKAT USA, Inc.
Date Deposited: 02 Nov 2021 10:58
Last Modified: 02 Nov 2021 11:00
DOI or ID number: 10.24820/ark.5550190.p011.646
URI: https://researchonline.ljmu.ac.uk/id/eprint/15722
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