Combined NK1 and NK2 tachykinin receptor antagonists: Synthesis and structure-activity relationships of novel oxazolidine analogues

Article abstract of DOI:10.1016/S0960-894X(99)00093-1

We report herein the synthesis and structure-activity relationships of a series of novel oxazolidine analogues with regards to NK₁ and NK₂ tachykinin receptor binding affinity. Among this series of oxazolidine analogues, some compounds exhibited excellent high binding affinities for both NK₁ and NK₂ receptors. In addition, we describe the inhibitory effect in vivo on SP-induced airway vascular hyperpermeability and NKA-induced bronchoconstriction in guinea pigs.