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TitleSubstituted pyrazoles as hepatoselective HMG-CoA reductase inhibitors: discovery of (3R,5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl)-2H-pyrazol-3-yl]-3,5-dihydroxyheptanoic acid (PF-3052334) as a candidate for the treatment of hypercholesterolemia.
Journal, issue, pagesJ. Med. Chem., Vol. 51, Page 31-45, Year 2008
Publish dateAug 31, 2007 (structure data deposition date)
AuthorsPfefferkorn, J.A. / Choi, C. / Larsen, S.D. / Auerbach, B. / Hutchings, R. / Park, W. / Askew, V. / Dillon, L. / Hanselman, J.C. / Lin, Z. ...Pfefferkorn, J.A. / Choi, C. / Larsen, S.D. / Auerbach, B. / Hutchings, R. / Park, W. / Askew, V. / Dillon, L. / Hanselman, J.C. / Lin, Z. / Lu, G.H. / Robertson, A. / Sekerke, C. / Harris, M.S. / Pavlovsky, A. / Bainbridge, G. / Caspers, N. / Kowala, M. / Tait, B.D.
External linksJ. Med. Chem. / PubMed:18072721
MethodsX-ray diffraction
Resolution1.7 Å
Structure data

PDB-2r4f:
Substituted Pyrazoles as Hepatselective HMG-COA reductase inhibitors
Method: X-RAY DIFFRACTION / Resolution: 1.7 Å

Chemicals

ChemComp-SO4:
SULFATE ION

ChemComp-RIE:
(3R,5R)-7-[1-(4-fluorophenyl)-4-(1-methylethyl)-3-{methyl[(1R)-1-phenylethyl]carbamoyl}-1H-pyrazol-5-yl]-3,5-dihydroxyheptanoic acid

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsOXIDOREDUCTASE / CHOLESTEROL / BIOCYNTHESIS / HMG-COA / NADPH / STATIN / Alternative splicing / Cholesterol biosynthesis / Endoplasmic reticulum / Glycoprotein / Lipid synthesis / Membrane / Peroxisome / Polymorphism / Steroid biosynthesis / Sterol biosynthesis / Transmembrane

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