2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion.

Sayer, James R; Walldén, Karin; Pesnot, Thomas; Campbell, Frederick; Gane, Paul J; Simone, Michela; Koss, Hans; Buelens, Floris; Boyle, Timothy P; Selwood, David L; Waksman, Gabriel; Tabor, Alethea B

Sayer, James R; Walldén, Karin; Pesnot, Thomas; Campbell, Frederick; Gane, Paul J; Simone, Michela; Koss, Hans; Buelens, Floris; Boyle, Timothy P; Selwood, David L; Waksman, Gabriel; Tabor, Alethea B.

Affiliation

Sayer JR; Department of Chemistry, UCL, 20, Gordon Street, London WC1H 0AJ, UK.
Walldén K; Institute of Structural and Molecular Biology, UCL and Birkbeck, Malet Street, London WC1E 7HX, UK.
Pesnot T; Department of Chemistry, UCL, 20, Gordon Street, London WC1H 0AJ, UK.
Campbell F; Department of Chemistry, UCL, 20, Gordon Street, London WC1H 0AJ, UK.
Gane PJ; Wolfson Institute for Biomedical Research, UCL, The Cruciform Building, Gower Street, London WC1E 6BT, UK.
Simone M; Wolfson Institute for Biomedical Research, UCL, The Cruciform Building, Gower Street, London WC1E 6BT, UK.
Koss H; Department of Chemistry, UCL, 20, Gordon Street, London WC1H 0AJ, UK.
Buelens F; Institute of Structural and Molecular Biology, UCL and Birkbeck, Malet Street, London WC1E 7HX, UK.
Boyle TP; Department of Chemistry, UCL, 20, Gordon Street, London WC1H 0AJ, UK.
Selwood DL; Wolfson Institute for Biomedical Research, UCL, The Cruciform Building, Gower Street, London WC1E 6BT, UK.
Waksman G; Institute of Structural and Molecular Biology, UCL and Birkbeck, Malet Street, London WC1E 7HX, UK.
Tabor AB; Department of Chemistry, UCL, 20, Gordon Street, London WC1H 0AJ, UK. Electronic address: a.b.tabor@ucl.ac.uk.

Bioorg Med Chem ; 22(22): 6459-70, 2014 Nov 15.

Article de En | MEDLINE | ID: mdl-25438770

ABSTRACT

ABSTRACT

A novel series of 8-amino imidazo[1,2-a]pyrazine derivatives has been developed as inhibitors of the VirB11 ATPase HP0525, a key component of the bacterial type IV secretion system. A flexible synthetic route to both 2- and 3-aryl substituted regioisomers has been developed. The resulting series of imidazo[1,2-a]pyrazines has been used to probe the structure-activity relationships of these inhibitors, which show potential as antibacterial agents.

Sujet(s)
Mots clés

8-Amino imidazo[1,2-a]pyrazine; ATPase inhibitor; Bacterial type IV secretion system; HP0525

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Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Sujet principal: Pyrazines / Protéines bactériennes / Imidazoles / Antibactériens Langue: En Journal: Bioorg Med Chem Sujet du journal: BIOQUIMICA / QUIMICA Année: 2014 Type de document: Article Pays d'affiliation: Royaume-Uni

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