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)

Full Text: HTML

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.

Related Compounds

  • 3-methylcrotonoyl...

Related Articles:

Fumigant toxicity and acetylcholinesterase inhibitory activity of 4 Asteraceae plant essential oils and their constituents against Japanese termite (Reticulitermes speratus Kolbe).

2014-07-01

[Pestic. Biochem. Physiol. 113 , 55-61, (2014)]

Reaction of silylketene acetals with 3, 3-dimethylacryloyl chloride. Rousseau G and Blanco L.

[Tetrahedron Lett. 26(35) , 4195-96, (1985)]

Structure and Biosynthesis of Chrysophysarin A, a Plasmodial Pigment from the Slime Mould Physarum polycephalum (Myxomycetes). Eisenbarth S and Steffan B.

[Tetrahedron 56(3) , 363-365, (2000)]

More Articles...