期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 15, 期 23, 页码 5293-5297出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.08.049
关键词
melanin concentrating hormone; obesity; aminoindazoles; palladium amination
The synthesis and biological evaluation of novel 3-amino indazole melanin concentrating hormone receptor-1 antagonists are reported, several of which demonstrated functional activity of less than 100 nM. Compounds 19 and 28, two of the more potent compounds identified in this study, were characterized by high exposure in the brain and demonstrated robust efficacy when dosed in diet-induced obese mice. (c) 2005 Published by Elsevier Ltd.
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