論文 - 詳細
| RRC ID | 71764 |
|---|---|
| 著者 | Konno H, Onuma T, Nitanai I, Wakabayashi M, Yano S, Teruya K, Akaji K. |
| タイトル | Synthesis and evaluation of phenylisoserine derivatives for the SARS-CoV 3CL protease inhibitor. |
| ジャーナル | Bioorg Med Chem Lett |
| Abstract |
Synthesis and evaluation of new scaffold phenylisoserine derivatives connected with the essential functional groups against SARS CoV 3CL protease are described. The phenylisoserine backbone was found by simulation on GOLD software and the structure activity relationship study of phenylisoserine derivatives gave SK80 with an IC50 value of 43μM against SARS CoV 3CL R188I mutant protease. |
| 巻・号 | 27(12) |
| ページ | 2746-2751 |
| 公開日 | 2017-6-15 |
| DOI | 10.1016/j.bmcl.2017.04.056 |
| PII | S0960-894X(17)30433-X |
| PMID | 28454669 |
| PMC | PMC7127027 |
| MeSH | Coronavirus 3C Proteases Cysteine Endopeptidases / genetics Cysteine Endopeptidases / metabolism Dose-Response Relationship, Drug Humans Models, Molecular Molecular Structure Protease Inhibitors / chemical synthesis Protease Inhibitors / chemistry Protease Inhibitors / pharmacology* Serine / analogs & derivatives* Serine / chemical synthesis Serine / chemistry Serine / pharmacology Structure-Activity Relationship Viral Proteins / antagonists & inhibitors* Viral Proteins / genetics Viral Proteins / metabolism |
| IF | 2.572 |
| リソース情報 | |
| ヒト・動物細胞 | HeLa(RCB0007) |