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 2024-01-20T18:04:38Z 2024-01-20T18:04:38Z 2021-09-04 2010-11-15 0960-894X https://pubs.kist.re.kr/handle/201004/130927 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. (C) 2010 Elsevier Ltd. All rights reserved. English Pergamon Press Ltd. RECEPTOR ANTAGONIST REUPTAKE INHIBITORS BIPOLAR DISORDER NEUROPSYCHOLOGY NEFAZODONE Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT2A, 5-HT2C, and the serotonin transporter as a potential antidepressant Article 10.1016/j.bmcl.2010.09.081 1 Bioorganic & Medicinal Chemistry Letters, v.20, no.22, pp.6439 - 6442 Bioorganic & Medicinal Chemistry Letters 20 22 6439 6442 scie scopus 000283052900019 2-s2.0-77958061381 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article RECEPTOR ANTAGONIST REUPTAKE INHIBITORS BIPOLAR DISORDER NEUROPSYCHOLOGY NEFAZODONE Antidepressant Serotonin Piperazine Pyrimidine