Title of article
Identification of 4-amino-2-cyclohexylaminoquinazolines as metabolically stable melanin-concentrating hormone receptor 1 antagonists Original Research Article
Author/Authors
Kosuke Kanuma، نويسنده , , Katsunori Omodera، نويسنده , , Mariko Nishiguchi، نويسنده , , Takeo Funakoshi، نويسنده , , Shigeyuki Chaki، نويسنده , , Yasuko Nagase، نويسنده , , Izumi Iida، نويسنده , , Jun-ichi Yamaguchi، نويسنده , , Graeme Semple، نويسنده , , Thuy-Anh Tran، نويسنده , , Yoshinori Sekiguchi، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
13
From page
3307
To page
3319
Abstract
The optimization of the distance between two key pharmacophore features within our first hit compounds 1a and 2a led to the identification of a new class of potent non-peptidic antagonists for the MCH-R1, based around 4-amino-2-cyclohexylaminoquinazolines. In particular, ATC0065 (2c), N2-[cis-4-({2-[4-Bromo-2-(trifluoromethoxy)phenyl]ethyl}amino)cyclohexyl]-N4,N4-dimethylquinazoline-2,4-diamine dihydrochloride, bound with high affinity to the MCH-R1 (IC50 value of 16 nM) and showed good metabolic stability in liver microsomes from human and rat.
Keywords
Melanin-concentrating hormone receptor 1 antagonists , MCH-R1 antagonists , ATC0065
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2006
Journal title
Bioorganic and Medicinal Chemistry
Record number
1305702
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