biostudies-literatureSayer JRWellcome TrustBiotechnology and Biological Sciences Research Council6459-70https://www.ebi.ac.uk/biostudies/studies/S-EPMC4339681biostudies-literatureUnknown22(22)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.Bioorganic & medicinal chemistry2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion.PMC4339681098302/Z/12/Z082227096617/Z/11/ZBBS/K/2005/12145BB/D005469/1(BBS/SE/2006/1326/9Koss HSimone MTabor ABGane PJWaksman GCampbell FBuelens FSelwood DLSayer JRPesnot TBoyle TPWallden Kfalse2- 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.2014-01-01T00:00:00Z2014 Nov2024-11-08T16:18:19.505Z2019-03-27T01:47:04ZS-EPMC43396812543877010.1016/j.bmc.2014.09.036