191673-32-2Relevant academic research and scientific papers
Combined tachykinin receptor antagonist: Synthesis and stereochemical structure-activity relationships of novel morpholine analogues
Nishi, Takahide,Ishibashi, Koki,Takemoto, Toshiyasu,Nakajima, Katsuyoshi,Fukazawa, Tetsuya,Iio, Yukiko,Itoh, Kazuhiro,Mukaiyama, Osamu,Yamaguchi, Takeshi
, p. 1665 - 1668 (2007/10/03)
We report herein the synthesis and stereochemical structure-activity relationships of novel morpholine analogues 12 and 13 with regards to NK1, NK2 and NK3 tachykinin receptor binding affinity. An essential requirement for more potent binding affinities was controlled by absolute configuration. (S,R)-12 and (S,R)-13 exhibited high binding affinities for NK1, NK2 and NK3 receptors. (C) 2000 Elsevier Science Ltd. All rights reserved.
Combined NK1 and NK2 tachykinin receptor antagonists: Synthesis and structure-activity relationships of novel oxazolidine analogues
Nishi, Takahide,Fukazawa, Tetsuya,Ishibashi, Koki,Nakajima, Katsuyoshi,Sugioka, Yuki,Iio, Yukiko,Kurata, Hitoshi,Itoh, Kazuhiro,Mukaiyama, Osamu,Satoh, Yumiko,Yamaguchi, Takeshi
, p. 875 - 880 (2007/10/03)
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.
An efficient synthesis of enantiomerically pure 2-[(2R)-arylmorpholin- 2-yl]ethanols, key intermediates of tachykinin receptor antagonist
Nishi, Takahide,Ishibashi, Koki,Nakajima, Katsuyoshi,Iio, Yukiko,Fukazawa, Tetsuya
, p. 3251 - 3262 (2007/10/03)
We report herein an efficient and practical synthetic method for the preparation of enantiomerically pure 2[(2R)-arylmorpholin-2-yl]ethanols 1a- d, key intermediates of tachykinin receptor antagonist. Sharpless catalytic asymmetric dihydroxylation of 4a-d was employed to introduce the required absolute stereochemistry, and cyclization of 7a-d was accomplished by the Mitsunobu reaction.
