Full metadata record
DC Field | Value | Language |
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dc.contributor.author | 정낙신 | - |
dc.date.accessioned | 2017-01-05T02:01:03Z | - |
dc.date.available | 2017-01-05T02:01:03Z | - |
dc.date.issued | 2008 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.other | OAK-4629 | - |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/233590 | - |
dc.description.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. | - |
dc.language | English | - |
dc.title | Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor | - |
dc.type | Article | - |
dc.relation.issue | 2 | - |
dc.relation.volume | 18 | - |
dc.relation.index | SCI | - |
dc.relation.index | SCIE | - |
dc.relation.index | SCOPUS | - |
dc.relation.startpage | 571 | - |
dc.relation.lastpage | 575 | - |
dc.relation.journaltitle | Bioorganic and Medicinal Chemistry Letters | - |
dc.identifier.doi | 10.1016/j.bmcl.2007.11.077 | - |
dc.identifier.wosid | WOS:000253410100024 | - |
dc.identifier.scopusid | 2-s2.0-38149132392 | - |
dc.author.google | Lee G.E. | - |
dc.author.google | Joshi B.V. | - |
dc.author.google | Chen W. | - |
dc.author.google | Jeong L.S. | - |
dc.author.google | Moon H.R. | - |
dc.author.google | Jacobson K.A. | - |
dc.author.google | Kim Y.-C. | - |
dc.contributor.scopusid | 정낙신(16028528200) | - |
dc.date.modifydate | 20211210153610 | - |