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Current Enzyme Inhibition


ISSN (Print): 1573-4080
ISSN (Online): 1875-6662

Recent Developments of Amidine-like Compounds as Selective NOS Inhibitors

Author(s): Nazzareno Re, Marialuigia Fantacuzzi, Cristina Maccallini, Roberto Paciotti and Rosa Amoroso

Volume 12, Issue 1, 2016

Page: [30 - 39] Pages: 10

DOI: 10.2174/1573408012999151109100557

Price: $65


The first generation of Nitric Oxide Synthases inhibitors was synthesized in the late 1980’s and early 1990’s; they were mainly amino acid derivatives, binding to the same residues within the enzyme heme-active site with respect to the natural substrate L-Arg, and showed no or scarce selectivity. In 1994, the N-(3-(aminomethyl)-benzyl) acetamidine (1400W), a highly selective compound for human iNOS versus both human eNOS and nNOS, was discovered. Following this landmark discover several other amidine-based iNOS and nNOS selective inhibitors have been disclosed. In this review we will focus on the recent progress and perspectives in the development of amidine-based selective iNOS and nNOS, including close analogues, with particular attention to acetamidine and aminopyridine derivatives.

Keywords: Acetamidine, amidine, 2-aminopyridine, nitric oxide synthases (NOS), NOS inhibitors.

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