2004
DOI: 10.1016/j.bmcl.2004.08.060
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Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity

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Cited by 6 publications
(3 citation statements)
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“…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 ).…”
Section: Resultsmentioning
confidence: 99%
See 1 more Smart Citation
“…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 ).…”
Section: Resultsmentioning
confidence: 99%
“…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.…”
Section: Discussionmentioning
confidence: 99%
“…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.…”
Section: S1 Commentmentioning
confidence: 99%