Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT2A, 5-HT2C, and the serotonin transporter as a potential antidepressant

作者：Kim Jong Yup; Kim Deukjoon^*; Kang Suk Youn; Park Woo Kyu; Kim Hyun Jung; Jung Myung Eun; Son Eun Jung; Pae Ae Nim; Kim Jeongmin; Lee Jinhwa

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(22): 6439-6442.

DOI：10.1016/j.bmcl.2010.09.081

• Antidepressant
• Serotonin
• Piperazine
• Pyrimidine

Pyrimidine usually has good pharmacokinetic properties as a drug substance and considerable efforts have been devoted to develop pyrimidine derivatives into drug candidates. Arylpiperazine-containing pyrimidine 4-carboxamide derivatives were synthesized and evaluated for binding to serotonin receptors and transporter. Pyrimidine derivatives showed good antidepressant activity in FST (forced swimming test) animal model and also displayed no appreciable inhibitory activity against hERG channel blocking assay. Herein SAR studies of pyrimidine derivatives targeting serotonin receptors and transporter will be disclosed.

• 出版日期2010-11-15