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期刊论文
Syntheses and Biological Activities of Ethyl N-Hydroxy-N-(substituted) phenyloxamates as KARI Inhibitors
CHEM. RES. CHINESE U. 2007, 23 (3), 280-283，-0001，（）：
Nine ethyl N-hydroxy-N-(substituted) phenyloxamates (2a-2i), based on the structure of the KARI inhibitor IpOHA, were synthesized. Their structures were established on the bases of 1H NMR, IR, ESI-MS and elemental analyses. Among the nine compounds, four show in vitro inhibitory activity on rice KARI, with 2c and 2g[Ki values of (35.2 ± 4.9) and (49.4 ± 6.3) μmol /L] having similar activity to the precursor of IpOHA (A, Ki = 34.1 ± 6.7 μmol /L). The results will be helpful to further molecular design of more potent KAR I inhibitors.
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