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Synthesis and Biological Evaluation of Disubstituted Pyrimidines as Selective 5-HT2C Agonists

Authors
Kim, JuhyeonKim, Yoon JungLondhe, Ashwini M.Pae, Ae NimChoo, HyunahKim, Hak JoongMin, Sun-Joon
Issue Date
9월-2019
Publisher
MDPI
Keywords
disubstituted pyrimidine; 5-HT2C receptor; cell-based assay; binding affinity; selectivity
Citation
MOLECULES, v.24, no.18
Indexed
SCIE
SCOPUS
Journal Title
MOLECULES
Volume
24
Number
18
URI
https://scholar.korea.ac.kr/handle/2021.sw.korea/63076
DOI
10.3390/molecules24183234
ISSN
1420-3049
Abstract
Here, we describe the synthesis of disubstituted pyrimidine derivatives and their biological evaluation as selective 5-HT2C agonists. To improve selectivity for 5-HT2C over other subtypes, we synthesized two series of disubstituted pyrimidines with fluorophenylalkoxy groups at either the 5-position or 4-position and varying cyclic amines at the 2-position. The in vitro cell-based assay and binding assay identified compounds 10a and 10f as potent 5-HT2C agonists. Further studies on selectivity to 5-HT subtypes and drug-like properties indicated that 2,4-disubstituted pyrimidine 10a showed a highly agonistic effect on the 5-HT2C receptor, with excellent selectivity, as well as exceptional drug-like properties, including high plasma and microsomal stability, along with low CYP inhibition. Thus, pyrimidine 10a could be considered a viable lead compound as a 5-HT2C selective agonist.
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