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Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor

Title
Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor
Authors
Lee G.E.Joshi B.V.Chen W.Jeong L.S.Moon H.R.Jacobson K.A.Kim Y.-C.
Ewha Authors
정낙신
Issue Date
2008
Journal Title
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894XJCR Link
Citation
vol. 18, no. 2, pp. 571 - 575
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
Analogues of the P2X7 receptor antagonist KN-62, modified at the piperazine and arylsulfonyl groups, were synthesized and assayed at the human P2X7 receptor for inhibition of BzATP-induced effects, that is, uptake of a fluorescent dye (ethidium bromide) in stably transfected HEK293 cells and IL-1β release in differentiated THP-1 cells. Substitution of the arylsulfonyl moiety with a nitro group increased antagonistic potency relative to methyl substitution, such that compound 21 was slightly more potent than KN-62. Substitution with d-tyrosine in 36 and sterically bulky tyrosyl 3,5-dimethyl groups in 9 enhanced antagonistic potency. © 2007 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmcl.2007.11.077
Appears in Collections:
약학대학 > 약학과 > Journal papers
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