1142953-53-4Relevant academic research and scientific papers
Synthesis and pharmacological evaluation of aminopyrimidine series of 5-HT1A partial agonists
Dounay, Amy B.,Barta, Nancy S.,Bikker, Jack A.,Borosky, Susan A.,Campbell, Brian M.,Crawford, Terry,Denny, Lynne,Evans, Lori M.,Gray, David L.,Lee, Pil,Lenoir, Edward A.,Xu, Wenjian
, p. 1159 - 1163 (2009)
Aminopyrimidine 2 (4-(1-(2-(1H-indol-3-yl)ethyl)piperidin-3-yl)-N-cyclopropylpyrimidin-2-amine) emerged from a high throughput screen as a novel 5-HT1A agonist. This compound showed moderate potency for 5-HT1A in binding and functional assays, as well as moderate metabolic stability. Implementation of a strategy for improving metabolic stability by lowering the lipophilicity (c Log D) led to identification of methyl ether 31 (4-(1-(2-(1H-indol-3-yl)ethyl)piperidin-3-yl)-N-(2-methoxyethyl)pyrimidin-2-amine) as a substantially improved compound within the series.
