Abstract
Longstanding and firsthand infectious diseases are challenging community health threats. A new series of isatin derivatives bearing β-hydroxy ketone, chalcone, or spiro-heterocycle moiety, was synthesized in a good yield. Chemical structures of the synthesized compounds were elucidated using spectroscopic techniques and elemental analysis. Antibacterial activities of the compounds were then evaluated
and by
modeling. The compounds were more active against Gram-positive bacteria,
(
= 0.026-0.226 mmol L
) and
(
= 0.348-1.723 mmol L-1) than against Gram-negative bacteria (
= 0.817-7.393 mmol L
). Only 3-hydroxy-3-(2-(2,5-dimethylthiophen-3-yl)-2-oxoethyl)indolin-2-one (
) was found as active as imipenem against
(
= 0.026 mmol L
).
docking of the compounds in the binding sites of a homology modeled structure of
histidine kinase-Walk allowed us to shed light on the binding mode of these novel inhibitors. The highest antibacterial activity of
is consistent with its highest docking score values against
histidine kinase.