期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 3, 页码 662-667出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.10.098
关键词
N-type calcium channel; analgesia; thiazolidinone
A series of new N-type (Ca(v)2.2) calcium channel blockers derived from the 'hit' structures 2-(3-bromo-4-fluorophenyl)-3(2-pyridin-2-yiethyl)thiazolidin-4-one 9 and its 2-[4-(4-bromophenyl)pyridin-3-yl]-3-isobutyI analogue 10 is described. Extensive SAR studies using a range of synthetic approaches resulted in novel, patented compounds with IC50 values of up to 0.2 mu M in an in vitro IMR32 assay, and selectivities for N/L of up to 30-fold. The new compounds described have potential in treatment of neuropathic pain. (c) 2006 Elsevier Ltd. All rights reserved.
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