新型苯乙吡啶酮衍生物作为强效促黑素聚集激素1受体拮抗剂的发现。
Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.
作者信息
Ando Makoto, Sekino Etsuko, Haga Yuji, Moriya Minoru, Ito Masahiko, Ito Junko, Iwaasa Hisashi, Ishihara Akane, Kanatani Akio, Ohtake Norikazu
机构信息
Department of Medicinal Chemistry, Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co. Ltd, Okubo-3, Tsukuba, Ibaraki, Japan.
出版信息
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5186-90. doi: 10.1016/j.bmcl.2009.07.023. Epub 2009 Jul 9.
Novel phenethylpyridone derivatives were identified as potent human melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. A search for surrogates for the 4-(2-aminoethoxy)phenyl moiety of 1 resulted in discovery of 2-[4-(aminomethyl)phenyl]ethyl substructure as in 6a. Successive optimization of the right-hand moiety led to the identification of a number of potent derivatives.
新型苯乙吡啶酮衍生物被鉴定为强效的人黑色素浓缩激素1受体（MCH-1R）拮抗剂。对化合物1的4-(2-氨基乙氧基)苯基部分进行替代物搜索，结果发现了如化合物6a中的2-[4-(氨基甲基)苯基]乙基亚结构。对右侧部分的连续优化导致了一系列强效衍生物的鉴定。
Zotero 插件