2r4f: Difference between revisions

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[[Image:2r4f.~~jpg~~|left|200px]]

[[Image:2r4f.png|left|200px]]

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~~'''~~Substituted Pyrazoles as Hepatselective HMG-COA reductase inhibitors~~'''~~

===Substituted Pyrazoles as Hepatselective HMG-COA reductase inhibitors===

~~==Overview==~~

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~~In light of accumulating evidence that aggressive LDL-lowering therapy may offer increased protection against coronary heart disease~~, ~~we undertook~~ the design and synthesis of a novel series of HMG-CoA reductase inhibitors based upon a substituted pyrazole template. Optimizing this series using both structure-based design and molecular property considerations afforded a class of highly efficacious and hepatoselective inhibitors resulting in the ~~identification of~~ (~~3 R,5 R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl~~)~~-2 H-pyrazol-3-yl]-3~~,5-~~dihydroxy~~-~~heptanoic (PF-3052334) as a candidate for the treatment of hypercholesterolemia.~~

The line below this paragraph, {{ABSTRACT_PUBMED_18072721}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 18072721 is the PubMed ID number.

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==Disease==

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[[Category: Sterol biosynthesis]]

[[Category: Transmembrane]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Wed Apr 30 13~~:22:16 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 06:58:34 2008''

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-[[Image:2r4f.jpg|left|200px]]
+{{Seed}}
+[[Image:2r4f.png|left|200px]]
 <!--
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 {{STRUCTURE_2r4f|  PDB=2r4f  |  SCENE=  }}
-'''Substituted Pyrazoles as Hepatselective HMG-COA reductase inhibitors'''
+===Substituted Pyrazoles as Hepatselective HMG-COA reductase inhibitors===
-==Overview==
+<!--
-In light of accumulating evidence that aggressive LDL-lowering therapy may offer increased protection against coronary heart disease, we undertook the design and synthesis of a novel series of HMG-CoA reductase inhibitors based upon a substituted pyrazole template. Optimizing this series using both structure-based design and molecular property considerations afforded a class of highly efficacious and hepatoselective inhibitors resulting in the identification of (3 R,5 R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl)-2 H-pyrazol-3-yl]-3,5-dihydroxy-heptanoic (PF-3052334) as a candidate for the treatment of hypercholesterolemia.
+The line below this paragraph, {{ABSTRACT_PUBMED_18072721}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 18072721 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_18072721}}
 ==Disease==
@@ Line 46: / Line 50: @@
 [[Category: Sterol biosynthesis]]
 [[Category: Transmembrane]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Apr 30 13:22:16 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 06:58:34 2008''