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
基金Supported by the National Basic Research Program of China(No2003CB114406)the National Natural Science Foundationof China(Key Project No20432010)
文摘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.
