Abstract
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.
Current Enzyme Inhibition
Title:Recent Developments of Amidine-like Compounds as Selective NOS Inhibitors
Volume: 12 Issue: 1
Author(s): Nazzareno Re, Marialuigia Fantacuzzi, Cristina Maccallini, Roberto Paciotti and Rosa Amoroso
Affiliation:
Keywords: Acetamidine, amidine, 2-aminopyridine, nitric oxide synthases (NOS), NOS inhibitors.
Abstract: 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.
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Cite this article as:
Re Nazzareno, Fantacuzzi Marialuigia, Maccallini Cristina, Paciotti Roberto and Amoroso Rosa, Recent Developments of Amidine-like Compounds as Selective NOS Inhibitors, Current Enzyme Inhibition 2016; 12 (1) . https://dx.doi.org/10.2174/1573408012999151109100557
DOI https://dx.doi.org/10.2174/1573408012999151109100557 |
Print ISSN 1573-4080 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6662 |
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