- Title
- 2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion
- Creator
- Sayer, James R.; Walldén, Karin; Waksman, Gabriel; Tabor, Alethea B.; Pesnot, Thomas; Campbell, Frederick; Gane, Paul J.; Simone, Michela; Koss, Hans; Buelens, Floris; Boyle, Timothy P.; Selwood, David L.
- Relation
- Bioorganic and Medicinal Chemistry Vol. 22, Issue 22, p. 6459-6470
- Publisher Link
- http://dx.doi.org/10.1016/j.bmc.2014.09.036
- Publisher
- Elsevier
- Resource Type
- journal article
- Date
- 2014
- Description
- 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.
- Subject
- 8-Amino imidazo[1,2-a]pyrazine; bacterial type IV secretion system; HP0525; ATPase inhibitor
- Identifier
- http://hdl.handle.net/1959.13/1065975
- Identifier
- uon:18018
- Identifier
- ISSN:0968-0896
- Language
- eng
- Full Text
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