Collect. Czech. Chem. Commun. 1998, 63, 103-114

2,4-Dihydroxyacetophenone Derivatives as Antileukotrienics with a Multiple Activity Mechanism

Miroslav Kuchař, Kateřina Čulíková, Vladimíra Panajotovová, Bohumila Brunová, Antonín Jandera and Vojtěch Kmoníček

Research Institute for Pharmacy and Biochemistry, 130 60 Prague 3, Czech Republic


A series of 2,4-dihydroxy-3-propylacetophenone derivatives containing alkylthiobenzoic or arylacetic acid moiety was prepared. The antileukotrienic activity of the substances was assessed in terms of inhibition of the biosynthesis of LTB4 and bonding to LTB4 and LTD4 receptors. Some of the substances were found to exert a complex antileukotrienic effect in all of the three tests. The compounds also displayed an antiinflammatory effect, as manifested by a significant inhibition of LTD4-induced bronchospasm.

Keywords: 2,4-Dihydroxy-3-propylacetophenone derivatives; Antileukotrienic activity; Antiasthmatic effect.