Bioorganic and Medicinal Chemistry Letters p. 875 - 880 (1999)
Update date:2022-08-05
Topics:
Nishi, Takahide
Fukazawa, Tetsuya
Ishibashi, Koki
Nakajima, Katsuyoshi
Sugioka, Yuki
Iio, Yukiko
Kurata, Hitoshi
Itoh, Kazuhiro
Mukaiyama, Osamu
Satoh, Yumiko
Yamaguchi, Takeshi
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.
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