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Design, synthesis, and anti-RNA virus activity of 6 '-Fluorinated-Aristeromycin analogues
DC Field | Value | Language |
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dc.contributor.author | Yoon, Ji-seong | - |
dc.contributor.author | Kim, Gyudong | - |
dc.contributor.author | Jarhad, Dnyandev B. | - |
dc.contributor.author | Kim, Hong-Rae | - |
dc.contributor.author | Shin, Young-Sup | - |
dc.contributor.author | Qu, Shuhao | - |
dc.contributor.author | Sahu, Pramod K. | - |
dc.contributor.author | Kim, Hea Ok | - |
dc.contributor.author | Lee, Hyuk Woo | - |
dc.contributor.author | Wan, Su Bin | - |
dc.contributor.author | Kong, Yun Jeong | - |
dc.contributor.author | Chang, Tong-Shin | - |
dc.contributor.author | Ogando, Natacha S. | - |
dc.contributor.author | Kovacikova, Kristina | - |
dc.contributor.author | Snijder, Eric J. | - |
dc.contributor.author | Posthuma, Clara C. | - |
dc.contributor.author | van Hemert, Martijn J. | - |
dc.contributor.author | Jeong, Lak Shin | - |
dc.creator | 창동신 | - |
dc.date.accessioned | 2020-01-23T07:43:33Z | - |
dc.date.available | 2020-04-05T07:43:33Z | - |
dc.date.created | 2019-07-29 | - |
dc.date.issued | 2019-07-11 | - |
dc.identifier.citation | Journal of Medicinal Chemistry, Vol.62 No.13, pp.6346-6362 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | https://hdl.handle.net/10371/164011 | - |
dc.description.abstract | The 6'-fluorinated aristeromycins were designed as dual-target antiviral compounds aimed at inhibiting both the viral RNA-dependent RNA polymerase (RdRp) and the host cell S-adenosyl-L-homocysteine (SAH) hydrolase, which would indirectly target capping of viral RNA. The introduction of a fluorine at the 6'-position enhanced the inhibition of SAH hydrolase and the activity against RNA viruses. The adenosine and N-6-methyladenosine analogues 2a-e showed potent inhibition against SAH hydrolase, while only the adenosine derivatives 2a-c exhibited potent antiviral activity against all tested RNA viruses such as Middle East respiratory syndrome-coronavirus (MERS-CoV), severe acute respiratory syndrome-coronavirus, chikungunya virus, and/or Zika virus. 6',6'-Difluoroaristeromycin (2c) showed the strongest antiviral effect for MERS-CoV, with a similar to 2.5 log reduction in infectious progeny titer in viral load reduction assay. The phosphoramidate prodrug 3a also demonstrated potent broad-spectrum antiviral activity, possibly by inhibiting the viral RdRp. This study shows that 6'-fluorinated aristeromycins can serve as starting points for the development of broad-spectrum antiviral agents that target RNA viruses. | - |
dc.language | 영어 | - |
dc.language.iso | ENG | en |
dc.publisher | American Chemical Society | - |
dc.title | Design, synthesis, and anti-RNA virus activity of 6 '-Fluorinated-Aristeromycin analogues | - |
dc.type | Article | - |
dc.identifier.doi | 10.1021/acs.jmedchem.9b00781 | - |
dc.citation.journaltitle | Journal of Medicinal Chemistry | - |
dc.identifier.wosid | 000475543300025 | - |
dc.identifier.scopusid | 2-s2.0-85068313505 | - |
dc.description.srnd | OAIID:RECH_ACHV_DSTSH_NO:T201918484 | - |
dc.description.srnd | RECH_ACHV_FG:RR00200001 | - |
dc.description.srnd | ADJUST_YN: | - |
dc.description.srnd | EMP_ID:A080898 | - |
dc.description.srnd | CITE_RATE:6.054 | - |
dc.description.srnd | DEPT_NM:약학과 | - |
dc.description.srnd | EMAIL:changts@snu.ac.kr | - |
dc.description.srnd | SCOPUS_YN:Y | - |
dc.citation.endpage | 6362 | - |
dc.citation.number | 13 | - |
dc.citation.startpage | 6346 | - |
dc.citation.volume | 62 | - |
dc.description.isOpenAccess | Y | - |
dc.contributor.affiliatedAuthor | Chang, Tong-Shin | - |
dc.contributor.affiliatedAuthor | Jeong, Lak Shin | - |
dc.identifier.srnd | T201918484 | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.subject.keywordPlus | L-CYCLOPENTENONE DERIVATIVES | - |
dc.subject.keywordPlus | MECHANISM-BASED INHIBITORS | - |
dc.subject.keywordPlus | CHIKUNGUNYA VIRUS | - |
dc.subject.keywordPlus | CARBOCYCLIC NUCLEOSIDES | - |
dc.subject.keywordPlus | BIOLOGICAL EVALUATION | - |
dc.subject.keywordPlus | SEXUAL TRANSMISSION | - |
dc.subject.keywordPlus | PROTIDE TECHNOLOGY | - |
dc.subject.keywordPlus | NEPLANOCIN-A | - |
dc.subject.keywordPlus | ZIKA VIRUS | - |
dc.subject.keywordPlus | ADENOSINE | - |
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