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2000
Volume 12, Issue 1
  • ISSN: 1573-4080
  • E-ISSN: 1875-6662

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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/content/journals/cei/10.2174/1573408012999151109100557
2016-04-01
2025-06-16
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/content/journals/cei/10.2174/1573408012999151109100557
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  • Article Type:
    Research Article
Keyword(s): 2-aminopyridine; Acetamidine; amidine; nitric oxide synthases (NOS); NOS inhibitors
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