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Combined tachykinin receptor antagonist: synthesis and stereochemical structure-activity relationships of novel morpholine analogues.

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Nishi T,Ishibashi K,Takemoto T,Nakajima K,Fukazawa T,Iio Y,Itoh K,Mukaiyama O,Yamaguchi T

doi

10.1016/s0960-894x(00)00324-3

subject

Has Abstract

pub_date

2000-08-07 00:00:00

pages

1665-8

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(00)00324-3

journal_volume

10

pub_type

杂志文章

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