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Synthesis and structure-activity relationships of novel, substituted 5,6-dihydrodibenzo[a,g]quinolizinium P2X(7) antagonists

Authors
Lee, Ga EunLee, Ho-SungLee, So DeokKim, Jung-HoKim, Won-KiKim, Yong-Chul
Issue Date
1-Feb-2009
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Keywords
Iminium quaternary protoberberine alkaloids; Human P2X(7) receptor; Antagonist; Ethidium uptake; IL-1 beta release
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.19, no.3, pp 954 - 958
Pages
5
Indexed
SCIE
SCOPUS
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume
19
Number
3
Start Page
954
End Page
958
URI
https://scholar.korea.ac.kr/handle/2021.sw.korea/120600
DOI
10.1016/j.bmcl.2008.11.088
ISSN
0960-894X
1464-3405
Abstract
Iminium quaternary protoberberine alkaloids (QPA) have been found to be novel P2X(7) antagonists. To assess their structure-activity relationships, these compounds were modified at their R-1 and R-2 groups and assayed for their ability to inhibit the 2'(3')-O-(4-benzoylbenzoyl)-ATP (BzATP)-induced uptake of fluorescent ethidium by HEK-293 cells stably expressing the human P2X(7) receptor, and their ability to inhibit BzATP-induced IL-1 beta release by differentiated THP-1 cells. Compounds 15a and 15d, with alkyl groups at the R-1 position, and especially compound 19h, with the 2-NO2-4,5-dimethoxy-benzyl group at the R-2 position, had potent inhibitory efficacy as P2X(7) antagonists. (C) 2008 Elsevier Ltd. All rights reserved.
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