887703-74-4Relevant articles and documents
Substituted 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
Pfefferkorn, Jeffrey A.,Choi, Chulho,Larsen, Scott D.,Auerbach, Bruce,Hutchings, Richard,Park, William,Askew, Valerie,Dillon, Lisa,Hanselman, Jeffrey C.,Lin, Zhiwu,Lu, Gina H.,Robertson, Andrew,Sekerke, Catherine,Harris, Melissa S.,Pavlovsky, Alexander,Bainbridge, Graeme,Caspers, Nicole,Kowala, Mark,Tait, Bradley D.
, p. 31 - 45 (2008/09/20)
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 (3R,5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzyl- carbamoyl)-2H-pyrazol-3-yl]-3,5-dihydroxy-heptanoic (PF-3052334) as a candidate for the treatment of hypercholesterolemia.
