Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists

We report here new chemical series acting as antagonists of melanin-concentrating hormone receptor 1 (MCHR-1). Synthesis and structure–activity relationships are described leading to the identification of compounds with optimized in vitro pharmacological and in vitro ADME profiles. In vivo activity...

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Published inBioorganic & medicinal chemistry letters Vol. 17; no. 13; pp. 3754 - 3759
Main Authors Balavoine, Fabrice, Malabre, Patrice, Alleaume, Thierry, Rey, Astrid, Cherfils, Valérie, Jeanneton, Olivier, Seigneurin-Venin, Sophie, Revah, Frédéric
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 01.07.2007
Elsevier
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Summary:We report here new chemical series acting as antagonists of melanin-concentrating hormone receptor 1 (MCHR-1). Synthesis and structure–activity relationships are described leading to the identification of compounds with optimized in vitro pharmacological and in vitro ADME profiles. In vivo activity has been demonstrated in animal models of food intake and depression. We report here new chemical series acting as antagonists of melanin-concentrating hormone receptor 1 (MCHR-1). Synthesis and structure–activity relationships are described leading to the identification of compounds with optimized in vitro pharmacological and in vitro ADME profiles. In vivo activity has been demonstrated in animal models of food intake and depression.
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ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.04.012