Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity

…, L Bayless, X Cai, P Collart, JB Eckman, JL Ellis…

Index: Lewis, Timothy A.; Young, Michelle A.; Arrington, Mark P.; Bayless, Lynn; Cai, Xiong; Collart, Philippe; Eckman, Joseph B.; Ellis, James L.; Ene, Doina G.; Libertine, Lyn; Nicolas, Jean-Marie; Scannell, Ralph T.; Wels, Bruce F.; Wenberg, Karen; Wypij, Donna M. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 22 p. 5591 - 5594

Full Text: HTML

Citation Number: 8

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 ...