Synthesis and biological activity of 4,5-polymethylenepyrazole-derived HMG-COA reductase inhibitors |
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Authors: | Jin-Il Kim Young Hee Choi Yurngdong Jahng |
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Affiliation: | (1) College of Pharmacy, Yeungnam University, 712-749 Kyongsan, Korea |
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Abstract: | New HMG-CoA reductase inhibitors, in which 3-substituted 4,5-polymethylenepyrazoles are employed as a hydrophobic anchor connected to tetrahydro-4-hydroxy-2H-pyran-2-one by a two-carbon bridge, were designed and synthesized to exhibit significant inhibitory activity comparable to mevinolin. The most potent enzyme inhibitor (11cc, IC50=0.01 μM) is 4-fold more potent than lovastatin. |
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Keywords: | HMG-CoA reductase inhibitor 3-Substituted 4,5-polymethylenepyrazole |
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