Naslov
Synthesis and Anti-inflammatory Activity of Novel Furochromenes

Autori
Jivkov Elenkov, Ivaylo ; Hrvačić, Boška ; Marković, Stribor ; Mesić, Milan ; Čempuh Klonkay, Andreja ; Lerman, Lidija ; Filipović Sučić, Anita ; Vujasinović, Ines ; Bošnjak, Berislav ; Brajša, Karmen ; Žiher, Dinko ; Košutić Hulita, Nada ; Malnar, Ivica

Izvornik
Croatica chemica acta (0011-1643) 86 (2013), 3; 253-264

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
furochromenes; 4-hydroxycoumarins; mast cell degranulation; leukotriene B4; antiinflammatory activity; ear edema

Sažetak
A series of variously substituted furochromenes, hemiacetals 2, acetals 3, and rearranged compounds4, were synthesized from variously substituted 4-hydroxycoumarins and evaluated in several in vitro assays, inhibition of mast cell degranulation induced by the activation of Fcε receptor type I or calcium ionophore and leukotriene B4 (LTB4) inhibition. The most active derivatives, 3p and 4p (8-iso-propyl substitution in coumarin ring) and 3r (5-methyl-8-chloro substitution), showed significant inhibition of mast cell degranulation (Fctriggered) and LTB4, and exhibited significant local anti-inflammatory activity in PMA induced ear edema in CD1 mice, with potency equal (compounds 3p and 4p) or better (compound 3r) in comparison with zileuton, a reference drug used. It might be a promising direction for developing novel drugs as potential agents for the treatment of allergies and other inflammatory diseases

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA