Abstract

We report herein the synthesis and structure-activity relationships of a series of novel oxazolidine analogues with regards to NK 1 and NK 2 tachykinin receptor binding affinity. Among this series of oxazolidine analogues, some compounds exhibited excellent high binding affinities for both NK 1 and NK 2 receptors. In addition, we describe the inhibitory effect in vivo on SP-induced airway vascular hyperpermeability and NKA-induced bronchoconstriction in guinea pigs.

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