BMS-538203
| CAS号 | 543730-41-2 | 货号 | BCP10394 |
| 中文名 | BMS-538203 | ||
| 英文名 | BMS-538203 | ||
| 中文别名 | |||
| 英文别名 | BMS 538203;BMS538203; | ||
| 分子式 | C12H12FNO5 | 分子量 | 269.23 |
| 生物活性 | In the current study we demonstrate a hit-to-clinical candidate pathway that resulted in 50- and 2000-fold improvements in enzyme-inhibition and antiviral activity without an increase in molecular weight or change in molecular topology. The original hit , 1 (mw = 268) was optimized in a stepwise manner. Potential covalent protein-binding moieties were removed by reducing the number of the ketone groups. High enzyme inhibition activity was achieved by optimizing the aryl-portion of the molecule. Protein binding was reduced by replacing the standard amide by the corresponding methyl-hydroxamide. This eventually led to the discovery of BMS-538203 compound 2 (mw = 269) a highly efficient inhibitor and antiviral agent. | ||
| 信号通路 | Protease/Metabolic Enzyme Microbiology/Virology | ||
| 靶 点 | Integrase HIV | ||
结构式
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