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A rational approach to the design of a leukotriene antagonist.

Tudhope, Stephen Richard. (1987) A rational approach to the design of a leukotriene antagonist. Doctoral thesis, University of Surrey (United Kingdom)..

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Abstract

Leukotrienes are newly discovered metabolites of arachidonic acid believed to play a mediatory role in the pathogenesis of asthma. It was the intention, therefore to develop a leukotriene antagonist which may be clinically beneficial in this disease state. The known leukotrienes LT[C4], LTD[4], and LTE[4] were synthesised and studied in vitro on a range of animal tissues, which indicated the existence of three discrete leukotriene receptors. Synthesis of leukotriene analogues aimed at simplifying the agonist pharmacophore, resulted in the identification of a highly potent agonist of greater structural simplicity than the natural leukotrienes. From this starting point, using concepts of molecular rigidity and pharmacophoric group displacement, a compound was developed which antagonised the effects of the leukotrienes on the three receptor systems. This antagonist, bearing such a broad profile of activity, constitutes a major breakthrough in the field of leukotriene research.

Item Type: Thesis (Doctoral)
Divisions : Theses
Authors :
NameEmailORCID
Tudhope, Stephen Richard.
Date : 1987
Contributors :
ContributionNameEmailORCID
http://www.loc.gov/loc.terms/relators/THS
Additional Information : Thesis (Ph.D.)--University of Surrey (United Kingdom), 1987.
Depositing User : EPrints Services
Date Deposited : 22 Jun 2018 14:27
Last Modified : 06 Nov 2018 16:53
URI: http://epubs.surrey.ac.uk/id/eprint/848139

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