Synthesis of potential Rho-kinase inhibitors based on the chemistry of an original heterocycle: 4,4-Dimethyl-3,4-dihydro-1H-quinolin-2-one

A new series of substituted 4,4-dimethyl-3,4-dihydro-1H-quinolin-2-one have been prepared via condensation of 3,3-dimethylacryloyl chloride with aniline. Details of synthetic procedures are shown. Our aim was to investigate the potency of our original heterocycle in the inhibition of the Rho-kinase enzyme, known to be of major importance in the cascade reactions leading to arterial hypertension. Biological activity for the seven compounds has been investigated and is presented.

Graphical abstract A new series of substituted 4,4-dimethyl-3,4-dihydro-1H-quinolin-2-one have been synthesized. The seven compounds obtained were tested in the inhibition of the Rho-kinase enzyme known to be of major importance in the cascade reactions leading to arterial hypertension.Figure optionsDownload full-size imageDownload as PowerPoint slide