Synthesis and anti-measles virus activity of new isoquinolin-4-one derivatives.
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.
Santagati
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Dipartimento di Scienze Farmaceutiche, Facolta di Farmacia, Università degli Studi di Catania, Viale Andrea Doria, 6, 95125 Catania, Italy. santagat@unict.it
Bousquet
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E
Garozzo
A
A
Prezzavento
O
O
Spadaro
A
A
Ronsisvalle
G
G
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D008459:Measles virus / Q000187:drug effects* / Q000254:growth & development; D013329:Structure-Activity Relationship
D000998:Antiviral Agents; D007546:Isoquinolines; C039109:isoquinoline