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

Sayer, J.R. and Walldén, Karin and Pesnot, T. and Campbell, F. and Gane, P.J. and Simone, M. and Koss, H. and Buelens, Floris and Boyle, T.P. and Selwood, D.L. and Waksman, Gabriel and Tabor, A.B. (2014) 2- and 3-substituted imidazo [1,2-a] pyrazines as inhibitors of bacterial type IV secretion. Bioorganic & Medicinal Chemistry 22 (22), pp. 6459-6470. ISSN 0968-0896.

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.

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