Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 강수성 | * |
dc.date.accessioned | 2022-06-02T16:32:19Z | - |
dc.date.available | 2022-06-02T16:32:19Z | - |
dc.date.issued | 2022 | * |
dc.identifier.issn | 2470-1343 | * |
dc.identifier.other | OAK-31577 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/261357 | - |
dc.description.abstract | Cyclic alpha-aryl beta-dicarbonyl derivatives are important scaffolds in medicinal chemistry. Palladium-catalyzed coupling reactions of haloarenes were conducted with diverse five- to seven-membered cyclic beta-dicarbonyl derivatives including barbiturate, pyrazolidine-3,5-dione, and 1,4-diazepane-5,7-dione. The coupling reactions of various para- or meta-substituted aryl halides occurred efficiently when Pd(t-Bu3P)(2), Xphos, and Cs2CO3 were used under 1,4-dioxane reflux conditions. Although the couplings of ortho-substituted aryl halides with pyrazolidine-3,5-dione and 1,4-diazepane-5,7-dione were moderate, the coupling with barbiturate was limited. Using the optimized reaction conditions, we synthesized several 5-aryl barbiturates as new scaffolds of Ca(V)1.3 Ca2+ channel inhibitors. Among the synthesized molecules, 14e was the most potent Ca(V)1.3 inhibitor with an IC50 of 1.42 mu M. | * |
dc.language | English | * |
dc.publisher | AMER CHEMICAL SOC | * |
dc.title | Palladium-Catalyzed alpha-Arylation of Cyclic beta-Dicarbonyl Compounds for the Synthesis of Ca(V)1.3 Inhibitors | * |
dc.type | Article | * |
dc.relation.issue | 16 | * |
dc.relation.volume | 7 | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 14252 | * |
dc.relation.lastpage | 14263 | * |
dc.relation.journaltitle | ACS OMEGA | * |
dc.identifier.doi | 10.1021/acsomega.2c00889 | * |
dc.identifier.wosid | WOS:000812725900001 | * |
dc.identifier.scopusid | 2-s2.0-85129112194 | * |
dc.author.google | Yun, Jisu | * |
dc.author.google | Jeong, Dayeon | * |
dc.author.google | Xie, Zhong | * |
dc.author.google | Lee, Sol | * |
dc.author.google | Kim, Jiho | * |
dc.author.google | Surmeier, D. James | * |
dc.author.google | Silverman, Richard B. | * |
dc.author.google | Kang, Soosung | * |
dc.contributor.scopusid | 강수성(56177300500) | * |
dc.date.modifydate | 20240527115543 | * |