European Journal of Medicinal Chemistry 2008-01-01

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

Marie-Anne Letellier, Jérôme Guillard, Daniel-Henri Caignard, Gilles Ferry, Jean A. Boutin, Marie-Claude Viaud-Massuard, Marie-Anne Letellier, Jérôme Guillard, Daniel-Henri Caignard, Gilles Ferry, Jean A. Boutin, Marie-Claude Viaud-Massuard

Index: Eur. J. Med. Chem. 43(8) , 1730-6, (2008)

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Abstract

A new series of substituted 4,4-dimethyl-3,4-dihydro-1 H-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.