2. Academic Validation
  3. Phosphorus-containing inhibitors of HMG-CoA reductase. 2. Synthesis and biological activities of a series of substituted pyridines containing a hydroxyphosphinyl moiety

Phosphorus-containing inhibitors of HMG-CoA reductase. 2. Synthesis and biological activities of a series of substituted pyridines containing a hydroxyphosphinyl moiety

  • J Med Chem. 1991 Sep;34(9):2804-15. doi: 10.1021/jm00113a019.
J A Robl 1,  L A Duncan,  J Pluscec,  D S Karanewsky,  E M Gordon,  C P Ciosek Jr,  L C Rich,  V C Dehmel,  D A Slusarchyk,  T W Harrity
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543-4000.
PMID: 1895299 DOI: 10.1021/jm00113a019
Abstract

A series of 2,3,4,(5),6-substituted pyridines containing a hydroxyphosphinyl functionally have been prepared and were evaluated for their ability to inhibit the enzyme HMG-CoA reductase. Systematic substitution of both R1-R4 and X-Y led to compounds of type 3-6 with in vitro potency greater than that of mevinolin (Na salt).

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