期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 15, 页码 4371-4375出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.06.075
关键词
mGluR5 non-competitive antagonist; carbamoyloxime
Hit-to-lead optimization of a HTS hit led to new carbamoyloxime derivatives. After identification of an advanced hit (8d) the CYP enzyme inhibitory activity of this class of compounds was successfully eliminated. Systematic exploration of different parts of the advanced hit led us to some promising lead compounds with mGluR5 affinities comparable to that of MPEP. (C) 2010 Elsevier Ltd. All rights reserved.
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