862652-50-4Relevant academic research and scientific papers
Reduction of hERG inhibitory activity in the 4-piperidinyl urea series of H3 antagonists
Berlin, Michael,Lee, Yoon Joo,Boyce, Christopher W.,Wang, Yi,Aslanian, Robert,McCormick, Kevin D.,Sorota, Steve,Williams, Shirley M.,West Jr., Robert E.,Korfmacher, Walter
scheme or table, p. 2359 - 2364 (2010/08/20)
Structural features of the substituted 4-piperidinyl urea analogs 1, responsible for the H3 antagonist activity, have been identified. Structure-activity relationship of the H3 receptor affinity, hERG ion channel inhibitory activity and their separation is described. Preliminary pharmacokinetic evaluation of the compounds of the series is addressed.
Biaryl ureas as potent and orally efficacious melanin concentrating hormone receptor 1 antagonists for the treatment of obesity
Palani, Anandan,Shapiro, Sherry,McBriar, Mark D.,Clader, John W.,Greenlee, William J.,Spar, Brian,Kowalski, Timothy J.,Farley, Constance,Cook, John,Van Heek, Margaret,Weig, Blair,O'Neill, Kim,Graziano, Michael,Hawes, Brian
, p. 4746 - 4749 (2007/10/03)
Herein, we report a small molecule MCH-R1 antagonist which demonstrates oral efficacy in chronic rodent models. Substituted phenyl biaryl urea derivatives were synthesized and evaluated as MCH-R1 antagonists for the treatment of obesity. The structure-activity relationship studies in this series resulted in identification of urea 1 as a potent and selective MCH-R1 antagonist. Compound 1 exhibited oral efficacy in chronic (28 d) rodent models at 3-30 mpk showing significant reduction in food intake and weight gain relative to controls.
