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

Loratadine and Analogues: Discovery and Preliminary Structure–Activity Relationship of Inhibitors of the Amino Acid Transporter B0AT2

“…The first indication for different binding requirements of these two proteins was provided by desloratadine. This active metabolite of loratadine binds with approximately 100-fold higher affinity than the parent compound to the H 1 R, , but is only a very weak inhibitor of B 0 AT2 (Table ). To examine whether the activity ratio can be shifted in favor of B 0 AT2, we determined the affinity of selected B 0 AT2 inhibitors for the human H 1 R (Table ).…”

“…Loratadine analogues have also been described as inhibitors of 5-lipoxygenase, platelet-activating factor (PAF), , farnesyl protein transferase (FPT), and K 2p18.1 channels . However, the SAR for these biological targets clearly diverges from the SAR for B 0 AT2.…”

1-(3-Bromopropoxy)-4-iodobenzene

“…The title compound, (I), is an intermediate in the synthesis of the dual-function H 1 antagonist/5-LO inhibitor compounds (Lewis et al, 2004) which would provide a valuable alternative to the currently available therapies on asthma. A view of the molecular structure of (I) is shown in Fig.…”