Identification of Optically Active Pyrimidine Derivatives as Selective 5-HT2C Modulators

Title
Identification of Optically Active Pyrimidine Derivatives as Selective 5-HT2C Modulators
Author
민선준
Keywords
pyrimidine; optically active; enzymatic kinetic resolution; 5-HT2C receptor; binding affinity; selectivity
Issue Date
2017-08
Publisher
MDPI AG
Citation
MOLECULES, v. 22, No. 9, Article no. 1416
Abstract
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.
URI
http://www.mdpi.com/1420-3049/22/9/1416/htmhttp://repository.hanyang.ac.kr/handle/20.500.11754/72263
ISSN
1420-3049
DOI
10.3390/molecules22091416
Appears in Collections:
COLLEGE OF SCIENCE AND CONVERGENCE TECHNOLOGY[E](과학기술융합대학) > CHEMICAL AND MOLECULAR ENGINEERING(화학분자공학과) > Articles
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