Kim, Juhyeon Jo, Hanbyeol Lee, Hyunseung Choo, Hyunah Kim, Hak Joong Pae, Ae Nim Cho, Yong Seo Min, Sun-Joon 2024-01-20T00:33:38Z 2024-01-20T00:33:38Z 2021-09-05 2017-09 1420-3049 https://pubs.kist.re.kr/handle/201004/122329 A series of pyrimidine derivatives 4a-i were synthesized and evaluated for their binding affinities towards 5-HT2C receptors. With regard to designed molecules 4a-i, the influence of the size of alkyl ether and the absolute configuration of a stereogenic center on the 5-HT2C binding affinity and selectivity was studied. The most promising diasteromeric mixtures 4d and 4e were selected in the initial radioligand binding assay and they were further synthesized as optically active forms starting from optically active alcohols 5d and 5e, prepared by an enzymatic kinetic resolution. Pyrimidine analogue (R,R)-4e displayed an excellent 5-HT2C binding affinity with good selectivity values against a broad range of other 5-HT receptor subtypes. English MDPI AG Identification of Optically Active Pyrimidine Derivatives as Selective 5-HT2C Modulators Article 10.3390/molecules22091416 1 MOLECULES, v.22, no.9 MOLECULES 22 9 N scie scopus 000411499400027 2-s2.0-85029613129 Biochemistry & Molecular Biology Chemistry, Multidisciplinary Biochemistry & Molecular Biology Chemistry Article SEROTONIN AGONISTS DESIGN SCHIZOPHRENIA VABICASERIN LORCASERIN MODELS pyrimidine optically active enzymatic kinetic resolution 5-HT2C receptor binding affinity selectivity