A new class of ibuprofen derivatives with reduced gastrotoxicity

Citation
Ml. Lolli et al., A new class of ibuprofen derivatives with reduced gastrotoxicity, J MED CHEM, 44(21), 2001, pp. 3463-3468
Citations number
29
Categorie Soggetti
Chemistry & Analysis
Journal title
JOURNAL OF MEDICINAL CHEMISTRY
ISSN journal
00222623 → ACNP
Volume
44
Issue
21
Year of publication
2001
Pages
3463 - 3468
Database
ISI
SICI code
0022-2623(20011011)44:21<3463:ANCOID>2.0.ZU;2-8
Abstract
A new series of nonsteroidal and inflammatory drugs (NSAIDs) obtained by li nking ibuprofen to selected furoxan moieties and to related furazans were s ynthesized and tested for their antiinflammatory, antiaggregatory, and ulce rogenic properties. All the derivatives are endowed with antiinflammatory a ctivity comparable to that of ibuprofen, but, unlike this drug, they displa y reduced acute gastrotoxicity. The masking of the ibuprofen-free carboxyli c group seems to be principally at the basis of this reduced topical irrita nt action. The two furoxan derivatives 8 and 9 also trigger potent antiaggr egatory effects, principally as a consequence of their NO-donor ability.