SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF MACROCYCLIC FKBP LIGANDS

被引：10

作者：

LUENGO, JI ^{[1
]}

KONIALIANBECK, A ^{[1
]}

LEVY, MA ^{[1
]}

BRANDT, M ^{[1
]}

EGGLESTON, DS ^{[1
]}

HOLT, DA ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT,DEPT PHYS & STRUCT CHEM,KING OF PRUSSIA,PA 19406

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(01)80136-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A number of pipecolinate dilactones have been synthesized as simplified macrocyclic mimics of the binding domains in rapamycin (1) and FK506 (2). Crystallographic studies of these compounds indicate that the conformation of the pipecolinyl alpha-ketoamide region is preorganized for binding to FKBP. This is confirmed by the ability of these analogs to inhibit the FKBP cis-trans peptidyl-prolyl isomerase activity.

引用

页码：321 / 324

页数：4

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