Palmer, Rex A., Potter, Brian S., Leach, Michael J. ORCID: 0000-0002-9859-1325 and Chowdhry, Babur Z. (2007) X-ray crystallographic structures of neuroprotective pyrimidine derivatives: (I) the mesylate salt of BW1003C87 and (II) sipatrigine base. Journal of Chemical Crystallography, 37 (11). pp. 771-777. ISSN 1074-1542 (Print), 1572-8854 (Online) (doi:https://doi.org/10.1007/s10870-007-9248-z)

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Abstract

Drugs based on 5-phenyl-2,4 diamino pyrimidine and 6-phenyl-1,2,4 triazine derivatives are well known for their effects on the central nervous system. The study presented here provides detailed crystal structures of two pyrimidine derivatives which have neuroprotective properties in models of both grey and white matter ischemia. Recently published studies suggest that the compounds lamotrigine (a triazine derivative), and the two pyrimidines BW1003C87 (I) and sipatrigine (II) mediate their primary in vivo mode of action by inhibiting voltage-gated Na+ channels. The X-ray crystal structures will contribute valuable data for applications involving binding and modelling studies of the biological actions of these drugs.

Item Type:	Article
Uncontrolled Keywords:	central nervous system drugs, pyrimidines, lamotrigines, voltage-gated Na+ channel inhibitors, crystal structures and drug design
Subjects:	Q Science > QD Chemistry R Medicine > RM Therapeutics. Pharmacology
Faculty / School / Research Centre / Research Group:	Faculty of Engineering & Science Faculty of Education, Health & Human Sciences > School of Human Sciences (HUM)
Related URLs:	Publisher
Last Modified:	09 Oct 2021 04:46
URI:	http://gala.gre.ac.uk/id/eprint/2519

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