Literature DB >> 3634830

3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 4. Side chain ester derivatives of mevinolin.

W F Hoffman, A W Alberts, P S Anderson, J S Chen, R L Smith, A K Willard.   

Abstract

Modification of the 2(S)-methylbutyryl moiety of mevinolin led to a series of side chain ester derivatives. A systematic exploration of the structure-activity relationships showed that the introduction of an additional aliphatic group on the carbon alpha to the carbonyl group increased potency. This observation led to the synthesis of compound 16, which has about 2.5 times the intrinsic inhibitory activity of mevinolin.

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Year:  1986        PMID: 3634830     DOI: 10.1021/jm00155a040

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  28 in total

1.  Short- and long-term effects of lovastatin and pravastatin alone and in combination with cholestyramine on serum lipids, lipoproteins and apolipoproteins in primary hypercholesterolaemia.

Authors:  B G Jacob; W Möhrle; W O Richter; P Schwandt
Journal:  Eur J Clin Pharmacol       Date:  1992       Impact factor: 2.953

2.  In vitro and in vivo antiproliferative effects of simvastatin, an HMG-CoA reductase inhibitor, on human glioma cells.

Authors:  T Kikuchi; Y Nagata; T Abe
Journal:  J Neurooncol       Date:  1997-09       Impact factor: 4.130

3.  Engineering Saccharomyces cerevisiae for production of simvastatin.

Authors:  Carly M Bond; Yi Tang
Journal:  Metab Eng       Date:  2018-09-10       Impact factor: 9.783

4.  Efficient synthesis of simvastatin by use of whole-cell biocatalysis.

Authors:  Xinkai Xie; Yi Tang
Journal:  Appl Environ Microbiol       Date:  2007-02-02       Impact factor: 4.792

5.  Directed evolution and structural characterization of a simvastatin synthase.

Authors:  Xue Gao; Xinkai Xie; Inna Pashkov; Michael R Sawaya; Janel Laidman; Wenjun Zhang; Ralph Cacho; Todd O Yeates; Yi Tang
Journal:  Chem Biol       Date:  2009-10-30

Review 6.  Recent examples of novel secondary metabolites.

Authors:  A G Brown
Journal:  Folia Microbiol (Praha)       Date:  1995       Impact factor: 2.099

7.  Method Validation for Analysis of Simvastatin in Human Plasma Using Liquid Chromatography Tandem Mass Spectrometry (LC-MS-MS).

Authors:  Khaled M Alakhali
Journal:  J Clin Diagn Res       Date:  2013-12-15

8.  Short-term effects of treatment with simvastatin on testicular function in patients with heterozygous familial hypercholesterolaemia.

Authors:  K Purvis; A Tollefsrud; H Rui; E Haug; J Norseth; L Viksmoen; L Ose; H Lund
Journal:  Eur J Clin Pharmacol       Date:  1992       Impact factor: 2.953

9.  Rational improvement of simvastatin synthase solubility in Escherichia coli leads to higher whole-cell biocatalytic activity.

Authors:  Xinkai Xie; Inna Pashkov; Xue Gao; Jennifer L Guerrero; Todd O Yeates; Yi Tang
Journal:  Biotechnol Bioeng       Date:  2009-01-01       Impact factor: 4.530

10.  Purification and Characterization of a Lovastatin Esterase from Clonostachys compactiuscula.

Authors:  T G Schimmel; W S Borneman; M J Conder
Journal:  Appl Environ Microbiol       Date:  1997-04       Impact factor: 4.792

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