Several synthetic methods for hypolipidemic HMG-CoA reductase inhibitors were reviewed, including thepreparation of the side chains with the suitable groups such as aldehydo, acetylenyl, sulfonyl, phosphono or amino a...Several synthetic methods for hypolipidemic HMG-CoA reductase inhibitors were reviewed, including thepreparation of the side chains with the suitable groups such as aldehydo, acetylenyl, sulfonyl, phosphono or amino as well as thecondensation of these chains with the heteroaromatic compounds by Wittig-Hornor or Julia-Kocienski Olefination reaction.展开更多
HMG-CoA reductase converts HMG-CoA to mevalonate,with this catalysis constituting a committed step in the biosynthesis of cholesterol.So,it’s primary drone in treatment coronary artery disease.At present,several stat...HMG-CoA reductase converts HMG-CoA to mevalonate,with this catalysis constituting a committed step in the biosynthesis of cholesterol.So,it’s primary drone in treatment coronary artery disease.At present,several statins are available in the drug market,however,up to now the quantitative structure-activity relationship of all of known inhibitors hasn’t been reported.In order to provide a theoretical guide for the synthesis of novel inhibitors,the quantitative structure-activity relationship of the inhibitors of HMG-CoA reductase were performed by using 3D-QSAR approach: comparative molecular field analysis(CoMFA).The computed obtained CoMFA model with(q^2=0.4,) r^2=0.955,SE=0.110,F=85.335.It not only can be used to explain the structure-activity relationship of compound but also has powerful predictive ability.展开更多
文摘Several synthetic methods for hypolipidemic HMG-CoA reductase inhibitors were reviewed, including thepreparation of the side chains with the suitable groups such as aldehydo, acetylenyl, sulfonyl, phosphono or amino as well as thecondensation of these chains with the heteroaromatic compounds by Wittig-Hornor or Julia-Kocienski Olefination reaction.
文摘HMG-CoA reductase converts HMG-CoA to mevalonate,with this catalysis constituting a committed step in the biosynthesis of cholesterol.So,it’s primary drone in treatment coronary artery disease.At present,several statins are available in the drug market,however,up to now the quantitative structure-activity relationship of all of known inhibitors hasn’t been reported.In order to provide a theoretical guide for the synthesis of novel inhibitors,the quantitative structure-activity relationship of the inhibitors of HMG-CoA reductase were performed by using 3D-QSAR approach: comparative molecular field analysis(CoMFA).The computed obtained CoMFA model with(q^2=0.4,) r^2=0.955,SE=0.110,F=85.335.It not only can be used to explain the structure-activity relationship of compound but also has powerful predictive ability.
