Dow Robert L, Hadcock John R, Scott Dennis O, Schneider Steven R, Paight Ernest S, Iredale Philip A, Carpino Philip A, Griffith David A, Hammond Marlys, Dasilva-Jardine Paul
Pfizer Global Research and Development, Groton, CT 06340, USA.
Bioorg Med Chem Lett. 2009 Sep 15;19(18):5351-4. doi: 10.1016/j.bmcl.2009.07.130. Epub 2009 Aug 6.
A new series of CB(1) receptor antagonists incorporating an imidazole-based isosteric replacement for the hydrazide moiety of rimonabant (SR141716) is disclosed. Members of this imidazole series possess potent/selective binding to the rCB(1) receptor and exhibit potent hCB(1) functional activity. Isopropyl analog 9a demonstrated activity in the tetrad assay and was orally-active in a food intake model.
公开了一系列新的CB(1)受体拮抗剂，其包含基于咪唑的等排体取代利莫那班（SR141716）的酰肼部分。该咪唑系列的成员对重组CB(1)受体具有强效/选择性结合，并表现出强效的人CB(1)功能活性。异丙基类似物9a在四联试验中显示出活性，并且在食物摄入模型中具有口服活性。
