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Syntheses and Biological Activities of Ethyl N-Hydroxy-N-(substituted)phenyloxamates as KARI Inhibitors
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作者 WANG Bao-lei LI Zheng-ming LI Yong-hong WANG Su-hua 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2007年第3期280-283,共4页
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 1^H NMR, IR, ESI-MS and elementa... 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 1^H 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 KARI inhibitors. 展开更多
关键词 KARI inhibitor IpOHA phenyloxamate Synthesis Biological activity
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