Izvorni znanstveni članak

https://doi.org/10.5562/cca2240

Synthesis and Anti-inflammatory Activity of Novel Furochromenes

Ivaylo Jivkov Elenkov ; Fidelta Ltd., Prilaz baruna Filipovića 29, HR-10000 Zagreb, Croatia
Boška Hrvačić ; Fidelta Ltd., Prilaz baruna Filipovića 29, HR-10000 Zagreb, Croatia
Stribor Marković ; Institute of Immunology, Inc., Rockefellerova 2, HR-10000 Zagreb, Croatia
Milan Mesić ; Fidelta Ltd., Prilaz baruna Filipovića 29, HR-10000 Zagreb, Croatia
Andreja Čempuh Klonkay ; PLIVA Croatia Ltd, Prilaz baruna Filipovića 25, HR-10000 Zagreb, Croatia
Lidija Lerman ; PLIVA Croatia Ltd, Prilaz baruna Filipovića 25, HR-10000 Zagreb, Croatia
Anita Filipović Sučić ; Croatian Agency for Medicinal Products and Medical Devices, Ksaverska cesta 4, HR-10000 Zagreb, Croatia
Ines Vujasinović ; Fidelta Ltd., Prilaz baruna Filipovića 29, HR-10000 Zagreb, Croatia
Berislav Bošnjak ; Department of Dermatology, Division of Immunology, Allergy and Infectious Diseases, Experimental Allergy, Medical University of Vienna, Lazarettgasse 19, A-1090 Vienna, Austria
Karmen Brajša ; Fidelta Ltd., Prilaz baruna Filipovića 29, HR-10000 Zagreb, Croatia
Dinko Žiher ; Fidelta Ltd., Prilaz baruna Filipovića 29, HR-10000 Zagreb, Croatia
Nada Košutić Hulita ; PLIVA Croatia Ltd, Prilaz baruna Filipovića 25, HR-10000 Zagreb, Croatia
Ivica Malnar orcid.org/0000-0002-3226-4583 ; Croatian Agency for Medicinal Products and Medical Devices, Ksaverska cesta 4, HR-10000 Zagreb, Croatia

Sažetak

A series of variously substituted furochromenes, hemiacetals 2, acetals 3, and rearranged compounds 4, 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 calci-um 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.(doi: 10.5562/cca2240)

Ključne riječi

furochromenes; 4-hydroxycoumarins; mast cell degranulation; leukotriene B4; anti-inflammatory activity; ear edema

Hrčak ID:

111298

URI

https://hrcak.srce.hr/111298

Datum izdavanja:

20.11.2013.

Posjeta: 2.447 *