Health & Environmental Research Online (HERO)


Print Feedback Export to File
473861 
Journal Article 
3- 5-(4,5-dihydro-1H-imidazol-2-yl)-furan-2-yl phenylamine (amifuraline), a promising reversible and selective peripheral MAO-A Inhibitor 
Gentili, F; Pizzinat, N; Ordener, C; Marchal-Victorion, S; Maurel, A; Hofmann, R; Renard, P; Delagrange, P; Pigini, M; Parini, A; Giannella, M 
2006 
Yes 
Journal of Medicinal Chemistry
ISSN: 0022-2623
EISSN: 1520-4804 
49 
18 
5578-5586 
English 
16942031 
WOS:000240149000021 
On the basis of the observation that the central side effects of MAO inhibitors may represent a major limit for their use in pathological processes involving peripheral MAOs, we investigated the possibility of generating novel inhibitors able to target specifically peripheral MAOs. To address this issue, we designed compounds 7-28. From biological results, the 2-( 5-phenyl-furan-2-yl)-4,5-dihydro-1H-imidazole ( Furaline, 17) proved to be a suitable lead. In fact, in enzyme assays on homogenate preparation from rat liver and HEK cells expressing MAO-A or MAO-B, compounds possessing the frame of 17 behaved as selective and reversible MAO-A inhibitors. Interestingly, in in vivo studies the amino derivative 21 ( Amifuraline), endowed with good hydrophilic character, was able to significantly inhibit liver but not brain MAO-A. 
monoamine-oxidase b; hydrogen-peroxide generation; imidazoline; binding-sites; profile modulation; gene-expression; intact-cells; ligands; medications; serotonin; receptor