New diaminoether coumarinic derivatives with anti-inflammatory activity

Citation
Dj. Hadjipavlou-litina, New diaminoether coumarinic derivatives with anti-inflammatory activity, ARZNEI-FOR, 50(7), 2000, pp. 631-635
Citations number
21
Categorie Soggetti
Pharmacology & Toxicology
Journal title
ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
ISSN journal
00044172 → ACNP
Volume
50
Issue
7
Year of publication
2000
Pages
631 - 635
Database
ISI
SICI code
0004-4172(200007)50:7<631:NDCDWA>2.0.ZU;2-3
Abstract
Four coumarinyl-oxy-diamines were synthesized and tested as anti-inflammato ry agents, pKa and log P were theoretically calculated. These compounds wer e tested for their ability to interact with 1,1 -diphenyl-2-picrylhydrazyl stable free radical (DPPH), to inhibit proteolysis and soybean lipoxygenase (LOX) in vitro. They were found to inhibit proteolysis (82-90 %) and soybe an lipoxygenase activity (52-79 %) very significant. On the contrary, their reducing ability was found to be low (8-22 %). The effect of the synthesis ed compounds on inflammation using the carageenan-induced rat paw oedema mo del was studied. They showed a potent inhibitory effect on inflammation (37 -55 %). Both anti-inflammatory and antioxidant activities depended on some structural characteristics of the synthesised compounds.