Author/Authors :
Timothy A. Lewis، نويسنده , , Michelle A. Young، نويسنده , , Mark P. Arrington، نويسنده , , Lynn Bayless، نويسنده , , Xiong Cai، نويسنده , , Philippe Collart، نويسنده , , Joseph B. Eckman، نويسنده , , James L. Ellis، نويسنده , , Doina G. Ene، نويسنده , , Lyn Libertine، نويسنده , , Jean Marie Nicolas، نويسنده , , Ralph T. Scannell، نويسنده , , Bruce F. Wels، نويسنده , , Karen Wenberg، نويسنده , , Donna M. Wypij، نويسنده ,
Abstract :
A series of compounds possessing both H1 histamine receptor antagonist and 5-lipoxygenase (5-LO) inhibitory activities was synthesized. The H1-binding scaffolds of cetirizine, efletirizine, and loratadine were linked to a lipophilic N-hydroxyurea, the 5-LO inhibiting moiety of zileuton. Both activities were observed in vivo, as was increased CYP3A4 inhibition compared to their respective single-function drugs. Selected analogs in the series were shown to be orally active in guinea pig models.
Keywords :
H1 antihistamine , e-mail: timlewis1201@comcast.net , 5-LO inhibitor.* Corresponding author. Tel.: +1 508 460 5099
