84176-76-1Relevant articles and documents
Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities
Tang, Haifeng,Yan, Yan,Feng, Zhe,De Jesus, Reynalda K.,Yang, Lihu,Levorse, Dorothy A.,Owens, Karen A.,Akiyama, Taro E.,Bergeron, Raynald,Castriota, Gino A.,Doebber, Thomas W.,Ellsworth, Kenneth P.,Lassman, Michael E.,Li, Cai,Wu, Margaret S.,Zhang, Bei B.,Chapman, Kevin T.,Mills, Sander G.,Berger, Joel P.,Pasternak, Alexander
scheme or table, p. 6088 - 6092 (2010/11/18)
A new series of thiazole-substituted 1,1,1,3,3,3-hexafluoro-2-propanols were prepared and evaluated as malonyl-CoA decarboxylase (MCD) inhibitors. Key analogs caused dose-dependent decreases in food intake and body weight in obese mice. Acute treatment with these compounds also led to a drop in elevated blood glucose in a murine model of type II diabetes.
Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK1/NK2 receptor antagonists
Burkholder, Timothy P.,Kudlacz, Elizabeth M.,Maynard, George D.,Liu, Xiao-Gao,Le, Tieu-Binh,Webster, Mark E.,Horgan, Stephen W.,Wenstrup, David L.,Freund, David W.,Boyer, Fred,Bratton, Larry,Gross, Raymond S.,Knippenberg, Robert W.,Logan, Deborah E.,Jones, Bryan K.,Chen, Teng-Man,Geary, Julie L.,Correll, Melinda A.,Poole, J. Chuck,Mandagere, Arun K.,Thompson, Thomas N.,Hwang, Kin-Kai
, p. 2531 - 2536 (2007/10/03)
We recently described the synthesis and characterization of MDL 105,212, a non peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors. Here we report the synthesis and structure-activity relationships for a series of analogs of MDL 105,212 with regards to: NK1 and NK2 receptor binding affinity, physical-chemical characterization; in vitro absorption potential; in vitro metabolic stability; and efficacy in a capsaicin-challenge conscious guinea pig model after oral administration.
