3-Alkyl- and 3-amido-isothiazoloquinolin-4-ones as ligands for the benzodiazepine site of GABAA receptors

► 3-Alkyl- and 3-amido-6-methylisothiazoloquinolin-4-ones have been synthesized. ► They bind to the benzodiazepine binding site of the GABAA receptors. ► The most potent compounds have high affinity with Ki values in the low nM range.