Recent Developments of Amidine-like Compounds as Selective NOS Inhibitors

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

Journal Name: Current Enzyme Inhibition

Volume 12 , Issue 1 , 2016

Become EABM
Become Reviewer
Call for Editor


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.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2016
Page: [30 - 39]
Pages: 10
DOI: 10.2174/1573408012999151109100557

Article Metrics

PDF: 47
PRC: 1