Bioorganic & Medicinal Chemistry 2014-11-15

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

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

Index: Bioorg. Med. Chem. 22(22) , 6459-70, (2014)

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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. Copyright © 2014 The Authors. Published by Elsevier Ltd.. All rights reserved.