Sayer, James R.; Wallden, 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.
2-and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion
BIOORGANIC & MEDICINAL CHEMISTRY, 22:6459-6470, NOV 15 2014

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.

DOI:10.1016/j.bmc.2014.09.036

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