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Synthesis and structure-activity relationships of novel, substituted 5,6-dihydrodibenzo[a,g]quinolizinium P2X(7) antagonists
- Issue Date
- 1-2월-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
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 19
- Number
- 3
- Start Page
- 954
- End Page
- 958
- ISSN
- 0960-894X
- 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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