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. (c) 2007 Elsevier Masson SAS. All rights reserved.