3bgl: Difference between revisions

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{{STRUCTURE_3bgl|  PDB=3bgl  |  SCENE=  }}  
{{STRUCTURE_3bgl|  PDB=3bgl  |  SCENE=  }}  


'''Hepatoselectivity of Statins: Design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors'''
===Hepatoselectivity of Statins: Design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors===




==Overview==
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4-Sulfamoyl pyrroles were designed as novel hepatoselective HMG-CoA reductase inhibitors (statins) to reduce myalgia, a statin-induced adverse effect. The compounds were prepared via a [3+2] cycloaddition of a Munchnone with a sulfonamide-substituted alkyne. We identified compounds with greater selectivity for hepatocytes compared to L6-myocytes than rosuvastatin and atorvastatin. There was an inverse correlation of myocyte potencies and ClogP values. A number of analogs were effective at reducing cholesterol in acute and chronic in vivo models but they lacked sufficient chronic in vivo activity to warrant further development.
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{{ABSTRACT_PUBMED_18155906}}


==Disease==
==Disease==
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[[Category: Steroid biosynthesis]]
[[Category: Steroid biosynthesis]]
[[Category: Transmembrane]]
[[Category: Transmembrane]]
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