STRUCTURE-ACTIVITY STUDIES OF SYNTHETIC FKBP LIGANDS AS PEPTIDYL-PROLYL ISOMERASE INHIBITORS

被引：40

作者：

HOLT, DA

KONIALIANBECK, AL

OH, HJ

YEN, HK

ROZAMUS, LW

KROG, AJ

ERHARD, KF

ORTIZ, E

LEVY, MA

BRANDT, M

BOSSARD, MJ

LUENGO, JI

机构：

[1] Department of Medicinal Chemistry, SmithKline Beecham Pharmaceuticals, King of Prussia

来源：

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

关键词：

D O I：

10.1016/S0960-894X(01)80135-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of non-macrocyclic pipecolyl alpha-ketoamides were prepared and evaluated as FKBP cis-trans peptidyl-prolyl isomerase inhibitors. These compounds exhibited inhibition constants as low as 2 nM. Their design was based on a consideration of the common FKBP-binding elements of FK506 and rapamycin. Structure-activity relationships are discussed.

引用

页码：315 / 320

页数：6

共 15 条

[11] MOLECULAR RECOGNITION OF IMMUNOPHILINS AND IMMUNOPHILIN-LIGAND COMPLEXES
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[14] ATOMIC-STRUCTURE OF FKBP-FK506, AN IMMUNOPHILIN-IMMUNOSUPPRESSANT COMPLEX
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