期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 13, 期 4, 页码 973-983出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2004.11.044
关键词
adenosine receptors; nucleoside analogues; binding; efficacy
资金
- Intramural NIH HHS [Z01 DK031115-24] Funding Source: Medline
In this paper we investigated the influence on affinity, selectivity and intrinsic activity upon modification of the adenosine agonist scaffold at the 3- and 5'-positions of the ribofuranosyl moiety and the 2- and N-6-positions of the purine base. This resulted in the synthesis of various analogues, that is, 3-12 and 24-33, with good hA(3)AR selectivity and moderate-to-high affinities (as in 32, K-i = 27 nM). Interesting was the ability to tune the intrinsic activity depending on the substituent introduced at the 3'-position. (C) 2004 Elsevier Ltd. All rights reserved.
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