3bgl

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{{STRUCTURE_3bgl| PDB=3bgl | SCENE= }}
{{STRUCTURE_3bgl| PDB=3bgl | SCENE= }}
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'''Hepatoselectivity of Statins: Design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors'''
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===Hepatoselectivity of Statins: Design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors===
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==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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(as it appears on PubMed at http://www.pubmed.gov), where 18155906 is the PubMed ID number.
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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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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Apr 30 13:38:36 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 00:49:47 2008''

Revision as of 21:49, 28 July 2008

Image:3bgl.png

Template:STRUCTURE 3bgl

Contents

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

Template:ABSTRACT PUBMED 18155906

Disease

Known disease associated with this structure: Statins, attenuated cholesterol lowering by OMIM:[142910]

About this Structure

3BGL is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Hepatoselectivity of statins: design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors., Park WK, Kennedy RM, Larsen SD, Miller S, Roth BD, Song Y, Steinbaugh BA, Sun K, Tait BD, Kowala MC, Trivedi BK, Auerbach B, Askew V, Dillon L, Hanselman JC, Lin Z, Lu GH, Robertson A, Sekerke C, Bioorg Med Chem Lett. 2008 Feb 1;18(3):1151-6. Epub 2007 Dec 5. PMID:18155906

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