期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 20, 期 6, 页码 2091-2100出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.01.036
关键词
Bradykinin; B2 antagonist; Inflammation; GPCR; Residence time
资金
- Italian Ministry of University [RIF.506/DSPAR 98]
A series of alpha,alpha-cycloalkylglycine sulfonamide compounds of general formula 1 has previously been identified by our group as selective human B-2(hB(2)) receptor antagonists. Here we report the in vitro and in vivo BK antagonist activity of a further evolution of the series, consisting in compounds of the general formula 2, containing either an alkyl piperazine or a 4-alkyl piperidine ring bearing various positively charged groups (R'). These studies unexpectedly revealed quite a flat nanomolar/subnanomolar SAR for the binding affinity, while differences were seen in the in vitro functional activities. We propose that variations in the residence time may explain these results. (C) 2012 Elsevier Ltd. All rights reserved.
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