基于尿素的吲唑类化合物作为黑色素浓缩激素受体1拮抗剂用于治疗肥胖症的合成与评价
Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.
作者信息
Souers Andrew J, Gao Ju, Wodka Dariusz, Judd Andrew S, Mulhern Mathew M, Napier James J, Brune Michael E, Bush Eugene N, Brodjian Sevan J, Dayton Brian D, Shapiro Robin, Hernandez Lisa E, Marsh Kennan C, Sham Hing L, Collins Christine A, Kym Philip R
机构信息
Metabolic Disease Research, Abbott Laboratories, Abbott Park, IL 60064, USA.
出版信息
Bioorg Med Chem Lett. 2005 Jun 2;15(11):2752-7. doi: 10.1016/j.bmcl.2005.03.114.
A series of urea-based N-1-(2-aminoethyl)-indazoles was synthesized and evaluated for melanin-concentrating hormone receptor 1 (MCHr1) antagonism in both binding and functional assays. Several compounds that acted as MCHr1 antagonists were identified, and optimization afforded a compound with excellent binding affinity, good functional potency, and oral efficacy in a chronic model for weight loss in diet-induced obese mice.
合成了一系列基于尿素的N-1-(2-氨基乙基)-吲唑，并在结合试验和功能试验中对其进行了黑色素浓缩激素受体1（MCHr1）拮抗作用的评估。鉴定出了几种作为MCHr1拮抗剂的化合物，通过优化得到了一种在饮食诱导肥胖小鼠的慢性减肥模型中具有优异结合亲和力、良好功能效价和口服疗效的化合物。
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