Ontology highlight
ABSTRACT:
SUBMITTER: Charlton MH
PROVIDER: S-EPMC5807874 | biostudies-literature | 2018 Feb
REPOSITORIES: biostudies-literature
Charlton Michael H MH Aleksis Rihards R Saint-Leger Adélaïde A Gupta Arya A Loza Einars E Ribas de Pouplana Lluís L Kaula Ilze I Gustina Daina D Madre Marina M Lola Daina D Jaudzems Kristaps K Edmund Grace G Randall Christopher P CP Kime Louise L O'Neill Alex J AJ Goessens Wil W Jirgensons Aigars A Finn Paul W PW
ACS medicinal chemistry letters 20180118 2
<i>N</i>-Leucinyl benzenesulfonamides have been discovered as a novel class of potent inhibitors of <i>E. coli</i> leucyl-tRNA synthetase. The binding of inhibitors to the enzyme was measured by using isothermal titration calorimetry. This provided information on enthalpy and entropy contributions to binding, which, together with docking studies, were used for structure-activity relationship analysis. Enzymatic assays revealed that <i>N</i>-leucinyl benzenesulfonamides display remarkable selecti ...[more]