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Synthesis and anti-measles virus activity of new isoquinolin-4-one derivatives
Authors:Santagati N A  Bousquet E  Garozzo A  Prezzavento O  Spadaro A  Ronsisvalle G
Affiliation:Dipartimento di Scienze Farmaceutiche, Facolta di Farmacia, Università degli Studi di Catania, Viale Andrea Doria, 6, 95125 Catania, Italy. santagat@unict.it
Abstract:Despite intense efforts to increase vaccine coverage, measles virus (MV) still causes significant morbidity and mortality in the world sometimes as a results of severe, chronic and lethal diseases. In an effort to develop therapies to supplement immunization strategies a number of 1-oxo-2-[[(1E)-phenylmethylene]amino]-1,2-dihydroisoquinoline-4-carboxylic acid derivatives were synthesized and evaluated for anti-measles activity. The substituents on the aromatic ring were chosen in order to evaluate the influence of electron-withdrawing or electron-donating effects on the electronic density of the aromatic moiety. We also evaluated the introduction of a vinyl chain between the exocyclic nitrogen and phenyl moiety. The biological results allow to outline some preliminary considerations on structure-activity relationship.
Keywords:Isoquinolin-4-one derivatives   Synthesis   Structure-activity relationship   Anti-viral activity   Measles virus
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