Sayer, JR;
Walldén, K;
Pesnot, T;
Campbell, F;
Gane, PJ;
Simone, M;
Koss, H;
... Tabor, AB; + view all
(2014)
2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion.
Bioorganic and Medical Chemistry
, 22
(22)
pp. 6459-6470.
10.1016/j.bmc.2014.09.036.
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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.
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