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  • Title: Synthesis of potential Rho-kinase inhibitors based on the chemistry of an original heterocycle: 4,4-dimethyl-3,4-dihydro-1H-quinolin-2-one.
    Author: Letellier MA, Guillard J, Caignard DH, Ferry G, Boutin JA, Viaud-Massuard MC.
    Journal: Eur J Med Chem; 2008 Aug; 43(8):1730-6. PubMed ID: 18164518.
    Abstract:
    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.
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