| Literature DB >> 19147349 |
Amy B Dounay1, Nancy S Barta, Jack A Bikker, Susan A Borosky, Brian M Campbell, Terry Crawford, Lynne Denny, Lori M Evans, David L Gray, Pil Lee, Edward A Lenoir, Wenjian Xu.
Abstract
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-HT(1A) agonist. This compound showed moderate potency for 5-HT(1A) in binding and functional assays, as well as moderate metabolic stability. Implementation of a strategy for improving metabolic stability by lowering the lipophilicity (cLogD) 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.Entities:
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Year: 2008 PMID： 19147349 DOI： 10.1016/j.bmcl.2008.12.087
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823