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

Abstract：

:A series of compounds possessing both H(1) histamine receptor antagonist and 5-lipoxygenase (5-LO) inhibitory activities was synthesized. The H(1)-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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Lewis TA,Young MA,Arrington MP,Bayless L,Cai X,Collart P,Eckman JB,Ellis JL,Ene DG,Libertine L,Nicolas JM,Scannell RT,Wels BF,Wenberg K,Wypij DM

doi

10.1016/j.bmcl.2004.08.060

subject

Has Abstract

pub_date

2004-11-15 00:00:00

pages

5591-4

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)01089-3

journal_volume

14

pub_type

杂志文章

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