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Selective inhibition of inducible nitric oxide synthase by derivatives of acetamidine.

Medicinal chemistry (Shariqah (United Arab Emirates)) (2012-06-30)
Cristina Maccallini, Antonia Patruno, Alessandra Ammazzalorso, Barbara De Filippis, Marialuigia Fantacuzzi, Sara Franceschelli, Letizia Giampietro, Simona Masella, Maria Luisa Tricca, Rosa Amoroso
RÉSUMÉ

A new series of phenyl- and heteryl acetamidines were synthesized and evaluated as inhibitors of nitric oxide synthases (NOS). While the N-substitution of the acetamidine moiety with different heterocycles appears to completely destroy the activity, linking the phenyl core preserves it. Moreover, it was observed a strong dependence of the phenylacetamidines potency of action from the length of the alkyl chain that connects the aromatic ring to the acetamidine moiety.

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Sigma-Aldrich
Acetamidine hydrochloride, 95%