Literature DB >> 17574411

Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors.

Jeffrey A Pfefferkorn1, Chulho Choi, Yuntao Song, Bharat K Trivedi, Scott D Larsen, Valerie Askew, Lisa Dillon, Jeffrey C Hanselman, Zhiwu Lin, Gina Lu, Andrew Robertson, Catherine Sekerke, Bruce Auerbach, Alexander Pavlovsky, Melissa S Harris, Graeme Bainbridge, Nicole Caspers.   

Abstract

Using structure-based design, a novel series of conformationally restricted, pyrrole-based inhibitors of HMG-CoA reductase were discovered. Leading analogs demonstrated potent inhibition of cholesterol synthesis in both in vitro and in vivo models and may be useful for the treatment of hypercholesterolemia and related lipid disorders.

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Year:  2007        PMID: 17574411     DOI: 10.1016/j.bmcl.2007.05.097

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  Scalable and chromatography-free synthesis of 2-(2-formylalkyl)arenecarboxylic acid derivatives through the supramolecularly controlled hydroformylation of vinylarene-2-carboxylic acids.

Authors:  Paweł Dydio; Joost N H Reek
Journal:  Nat Protoc       Date:  2014-04-24       Impact factor: 13.491

2.  Synthesis of unsymmetrical 3,4-diaryl-3-pyrrolin-2-ones utilizing pyrrole Weinreb amides.

Authors:  Jessica G Greger; Sarah J P Yoon-Miller; Nathan R Bechtold; Scott A Flewelling; Jacob P MacDonald; Catherine R Downey; Eric A Cohen; Erin T Pelkey
Journal:  J Org Chem       Date:  2011-09-26       Impact factor: 4.354

Review 3.  The Importance of Medicinal Chemistry Knowledge in the Clinical Pharmacist's Education.

Authors:  João Paulo S Fernandes
Journal:  Am J Pharm Educ       Date:  2018-03       Impact factor: 2.047

4.  Exploration of virtual candidates for human HMG-CoA reductase inhibitors using pharmacophore modeling and molecular dynamics simulations.

Authors:  Minky Son; Ayoung Baek; Sugunadevi Sakkiah; Chanin Park; Shalini John; Keun Woo Lee
Journal:  PLoS One       Date:  2013-12-30       Impact factor: 3.240

5.  A fungal tolerance trait and selective inhibitors proffer HMG-CoA reductase as a herbicide mode-of-action.

Authors:  Joel Haywood; Karen J Breese; Jingjing Zhang; Mark T Waters; Charles S Bond; Keith A Stubbs; Joshua S Mylne
Journal:  Nat Commun       Date:  2022-09-22       Impact factor: 17.694

  5 in total

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