Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.

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Abstract

The macrophage infectivity potentiator (MIP) protein is a major virulence factor of Legionella pneumophila, the causative agent of Legionnaires' disease. MIP belongs to the FK506-binding proteins (FKBP) and is necessary for optimal intracellular survival and lung tissue dissemination of L. pneumophila. We aimed to identify new small-molecule inhibitors of MIP by starting from known FKBP12 ligands. Computational analysis, synthesis, and biological testing of pipecolic acid derivatives revealed a promising scaffold for new MIP inhibitors.

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Journal

Journal ID (iso-abbrev): J. Med. Chem.

Title: Journal of medicinal chemistry

Publisher: American Chemical Society (ACS)

ISSN (Electronic): 1520-4804

ISSN (Print): 0022-2623

Publication date (Electronic): Jan 13 2011

Volume: 54

Issue: 1

Affiliations

[1 ] Institute of Pharmacy and Food Chemistry, University of Würzburg, Würzburg, Germany.

Article

DOI: 10.1021/jm101156y

PubMed ID: 21142106

SO-VID: c8bfcde7-fca4-4619-ae00-4a400b85e275

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