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

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. (C) 2014 The Authors. Published by Elsevier Ltd.