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Title: A rational approach to the design of a leukotriene antagonist
Author: Tudhope, Stephen Richard
Awarding Body: University of Surrey
Current Institution: University of Surrey
Date of Award: 1987
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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.
Supervisor: Not available Sponsor: Not available
Qualification Name: Thesis (Ph.D.) Qualification Level: Doctoral
EThOS ID:  DOI: Not available