Structure-activity studies of synthetic FKBP ligands as peptidyl-prolyl isomerase inhibitors

Bioorganic & Medicinal Chemistry Letters
1994.0

Abstract

A series of non-macrocyclic pipecolyl a-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.

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