AZA-TRICYCLIC SUBSTANCE-P ANTAGONISTS

被引：24

作者：

LOWE, JA ^{[1
]}

DROZDA, SE ^{[1
]}

MCLEAN, S ^{[1
]}

BRYCE, DK ^{[1
]}

CRAWFORD, RT ^{[1
]}

SNIDER, RM ^{[1
]}

LONGO, KP ^{[1
]}

NAGAHISA, A ^{[1
]}

TSUCHIYA, I ^{[1
]}

机构：

[1] PFIZER INC,DIV CENT RES,DEPT MED BIOL,AICHI 47023,JAPAN

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1994年 / 37卷 / 18期

关键词：

D O I：

10.1021/jm00044a002

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and structure-activity relationships of a series of aza-tricyclic analogs of the quinuclidine substance P (SP) antagonist 1 are described. The SP receptor affinity of these compounds was found to vary according to the size of the new ring fused to the quinuclidine and the mode of fusion. Correlations between receptor affinity and (1) the steric bulk of the newly introduced ring fusion and (2) the dihedral angle between the benzhydryl and benzylamino substituents of these aza-tricyclic compounds were explored.

引用

页码：2831 / 2840

页数：10

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