Ontology highlight
ABSTRACT:
SUBMITTER: Ngo HX
PROVIDER: S-EPMC6528465 | biostudies-literature | 2018 Jun
REPOSITORIES: biostudies-literature
ACS infectious diseases 20180330 6
A common cause of resistance to kanamycin (KAN) in tuberculosis is overexpression of the enhanced intracellular survival (Eis) protein. Eis is an acetyltransferase that multiacetylates KAN and other aminoglycosides, rendering them unable to bind the bacterial ribosome. By high-throughput screening, a series of substituted 1,2,4-triazino[5,6 b]indole-3-thioether molecules were identified as effective Eis inhibitors. Herein, we purchased 17 and synthesized 22 new compounds, evaluated their potency ...[more]