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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; | ||
SMILES | |||
化学名称 | |||
分子式 | C12H12FNO5 | 分子量 | 269.23 |
纯度 | 98% | 配送 | 惯例下常温包邮 |
产品描述 | 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. |
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