Design and synthesis of C-2 substituted Thiazolo and Dihydrothiazolo ring-fused 2-Pyridones: pilicides with increased antivirulence activity

Design and synthesis of C-2 substituted Thiazolo and Dihydrothiazolo ring-fused 2-Pyridones : pilicides with increased antivirulence activity

Chorell, Erik, 1980- (author): Umeå universitet,Kemiska institutionen,Institute of Structural and Molecular Biology, University College London/Birkbeck, Malet Street, London WC1E 7HX, U.K.

Pinkner, Jerome S (author): Department of Molecular Microbiology, Washington University, School of Medicine, St. Louis, Missouri 63110, USA

Phan, Gilles (author): Institute of Structural and Molecular Biology, University College London/Birkbeck, Malet Street, London WC1E 7HX, U.K.

Buelens, Floris (author): Institute of Structural and Molecular Biology, University College London/Birkbeck, Malet Street, London WC1E 7HX, U.K.

Remaut, Han (author): Institute of Structural and Molecular Biology, University College London/Birkbeck, Malet Street, London WC1E 7HX, U.K.

Waksman, Gabriel (author): Institute of Structural and Molecular Biology, University College London/Birkbeck, Malet Street, London WC1E 7HX, U.K.

Hultgren, Scott J (author): Department of Molecular Microbiology, Washington University, School of Medicine, St. Louis, Missouri 63110, USA

(creator_code:org_t)

2010-06-30
2010
English.
In: Journal of Medicinal Chemistry. - Washington, USA : American Chemical Society. - 0022-2623 .- 1520-4804. ; 53:15, s. 5690-5695

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Abstract Subject headings

Pilicides block pili formation by binding to pilus chaperones and blocking their function in the chaperone/usher pathway in E. coli. Various C-2 substituents were introduced on the pilicide scaffold by design and synthetic method developments. Experimental evaluation showed that proper substitution of this position affected the biological activity of the compound. Aryl substituents resulted in pilicides with significantly increased potencies as measured in pili-dependent biofilm and hemagglutination assays. The structural basis of the PapD chaperone-pilicide interactions was determined by X-ray crystallography.

By the author/editor: Chorell, Erik, 1 ...; Pinkner, Jerome ...; Phan, Gilles; Edvinsson, Sofie; Buelens, Floris; Remaut, Han; show more...; Waksman, Gabriel; Hultgren, Scott ...; Almqvist, Fredri ...; show less...

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