Abstract
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.
Keywords: Nitric oxide, Nitric oxide synthase, Selective inducible NOS inhibitors, Acetamidines, heterocycles, inorganic, neurodegenerative diseases, cytokines, polysaccharides, amino acid
Medicinal Chemistry
Title:Selective Inhibition of Inducible Nitric Oxide Synthase by Derivatives of Acetamidine
Volume: 8 Issue: 6
Author(s): Cristina Maccallini, Antonia Patruno, Alessandra Ammazzalorso, Barbara De Filippis, Marialuigia Fantacuzzi, Sara Franceschelli, Letizia Giampietro, Simona Masella, Maria Luisa Tricca and Rosa Amoroso
Affiliation:
Keywords: Nitric oxide, Nitric oxide synthase, Selective inducible NOS inhibitors, Acetamidines, heterocycles, inorganic, neurodegenerative diseases, cytokines, polysaccharides, amino acid
Abstract: 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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Maccallini Cristina, Patruno Antonia, Ammazzalorso Alessandra, De Filippis Barbara, Fantacuzzi Marialuigia, Franceschelli Sara, Giampietro Letizia, Masella Simona, Luisa Tricca Maria and Amoroso Rosa, Selective Inhibition of Inducible Nitric Oxide Synthase by Derivatives of Acetamidine, Medicinal Chemistry 2012; 8 (6) . https://dx.doi.org/10.2174/1573406411208060991
DOI https://dx.doi.org/10.2174/1573406411208060991 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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