Novel 2-aminobenzothiazoles as selective neuronal nitric oxide synthase inhibitors

A series of substituted 2-aminobenzothiazole compounds have been synthesized and evaluated as nitric oxide synthase (NOS) inhibitors. Compound 14 shows activity in the nM range and is selective for the human neuronal NOS isoform. We have also evaluated the compounds against the rat NOS isoforms. For some of the compounds, there are significant differences in NOS inhibitory activities between the human and rat enzymes. For example, compound 10b has nM activity against the rat nNOS while low μM activity against the human nNOS.

Graphical abstractA novel series of 2-aminobenzothiazoles were synthesized and shown to be selective inhibitors of neuronal nitric oxide synthase (nNOS).Figure optionsDownload full-size imageDownload as PowerPoint slide