Novel 5-HT3 antagonists: indol-3-ylspiro (azabicycloalkane-3, 5'(4'H) oxazoles)

…, R Baker, C Kneen, R Herbert, J Moseley…

Index: Swain; Baker; Kneen; Herbert; Moseley; Saunders; Seward; Stevenson; Beer; Stanton; Watling; Ball Journal of Medicinal Chemistry, 1992 , vol. 35, # 6 p. 1019 - 1031

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Citation Number: 45

Abstract

The synthesis and biochemical evaluation of a series of spirofused indole oxazoline 5-HT3 antagonists is described in which the oxazoline ring acta as a bioisosteric replacement for esters and amides. The effect of substitution about the indole ring has shown the steric limitations of the aromatic binding site. Incorporation of a variety of azabicyclic systems within the rigid spirofused framework has allowed the definition of a binding model which ...