Synthesis and Biological Evaluation of Disubstituted Pyrimidines as Selective 5-HT2C Agonists
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Kim, Juhyeon | - |
dc.contributor.author | Kim, Yoon Jung | - |
dc.contributor.author | Londhe, Ashwini M. | - |
dc.contributor.author | Pae, Ae Nim | - |
dc.contributor.author | Choo, Hyunah | - |
dc.contributor.author | Kim, Hak Joong | - |
dc.contributor.author | Min, Sun-Joon | - |
dc.date.accessioned | 2021-09-01T07:47:42Z | - |
dc.date.available | 2021-09-01T07:47:42Z | - |
dc.date.created | 2021-06-18 | - |
dc.date.issued | 2019-09 | - |
dc.identifier.issn | 1420-3049 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/63076 | - |
dc.description.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. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | MDPI | - |
dc.subject | RECEPTOR AGONISTS | - |
dc.subject | IN-VITRO | - |
dc.subject | DESIGN | - |
dc.subject | BEHAVIOR | - |
dc.title | Synthesis and Biological Evaluation of Disubstituted Pyrimidines as Selective 5-HT2C Agonists | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Kim, Hak Joong | - |
dc.identifier.doi | 10.3390/molecules24183234 | - |
dc.identifier.scopusid | 2-s2.0-85071736554 | - |
dc.identifier.wosid | 000488830500026 | - |
dc.identifier.bibliographicCitation | MOLECULES, v.24, no.18 | - |
dc.relation.isPartOf | MOLECULES | - |
dc.citation.title | MOLECULES | - |
dc.citation.volume | 24 | - |
dc.citation.number | 18 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Biochemistry & Molecular Biology | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Biochemistry & Molecular Biology | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Multidisciplinary | - |
dc.subject.keywordPlus | RECEPTOR AGONISTS | - |
dc.subject.keywordPlus | IN-VITRO | - |
dc.subject.keywordPlus | DESIGN | - |
dc.subject.keywordPlus | BEHAVIOR | - |
dc.subject.keywordAuthor | disubstituted pyrimidine | - |
dc.subject.keywordAuthor | 5-HT2C receptor | - |
dc.subject.keywordAuthor | cell-based assay | - |
dc.subject.keywordAuthor | binding affinity | - |
dc.subject.keywordAuthor | selectivity | - |
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