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

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Sayer JR,Walldén K,Pesnot T,Campbell F,Gane PJ,Simone M,Koss H,Buelens F,Boyle TP,Selwood DL,Waksman G,Tabor AB

doi

10.1016/j.bmc.2014.09.036

subject

Has Abstract

pub_date

2014-11-15 00:00:00

pages

6459-70

issue

22

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(14)00682-8

journal_volume

22

pub_type

杂志文章

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