Synthesis and biological evaluation of 3-benzyl-1-methyl- and 1-methyl-3-phenyl-isothioureas as potential inhibitors of iNOS

Nicola Paesano; Stefania Marzocco; Caterina Vicidomini; Carmela Saturnino; Giuseppina Autore; Giovanni De Martino; Gianluca Sbardella

doi:10.1016/j.bmcl.2004.11.047

Synthesis and biological evaluation of 3-benzyl-1-methyl- and 1-methyl-3-phenyl-isothioureas as potential inhibitors of iNOS

Bioorg Med Chem Lett. 2005 Feb 1;15(3):539-43. doi: 10.1016/j.bmcl.2004.11.047.

Authors

Nicola Paesano¹, Stefania Marzocco, Caterina Vicidomini, Carmela Saturnino, Giuseppina Autore, Giovanni De Martino, Gianluca Sbardella

Affiliation

¹ Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, via Ponte Don Melillo, 84084 Fisciano, Salerno, Italy.

PMID: 15664809
DOI: 10.1016/j.bmcl.2004.11.047

Abstract

Novel benzyl- and phenyl-isothioureidic derivatives have been synthesised and evaluated as inhibitors of nitric oxide synthesis, induced in lipopolysaccharide (LPS)-activated J774.A1 macrophage cell line. The most potent iNOS inhibitor resulting was 1-methyl-3-phenyl-S-methyl isothiourea 5l.

MeSH terms

Animals
Cell Line
Dose-Response Relationship, Drug
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / pharmacology
Lipopolysaccharides
Macrophages / enzymology
Mice
Nitric Oxide Synthase / antagonists & inhibitors*
Nitric Oxide Synthase Type II
Structure-Activity Relationship
Thiourea / chemical synthesis*
Thiourea / pharmacology*

Substances

Enzyme Inhibitors
Lipopolysaccharides
Nitric Oxide Synthase
Nitric Oxide Synthase Type II
Nos2 protein, mouse
Thiourea