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Merck
  • Novel squalene-hopene cyclase inhibitors derived from hydroxycoumarins and hydroxyacetophenones.

Novel squalene-hopene cyclase inhibitors derived from hydroxycoumarins and hydroxyacetophenones.

Chemical & pharmaceutical bulletin (2004-10-07)
Giancarlo Cravotto, Gianni Balliano, Silvia Tagliapietra, Simonetta Oliaro-Bosso, Gian Mario Nano
摘要

Squalene-hopene cyclase (SHC) is a useful model enzyme for predicting molecular interactions with oxidosqualene cyclase (OSC). Structure--activity relationships were investigated for numerous coumarin-derived inhibitors of SHC, and structural simplifications are suggested. Both umbelliferone and 2,4-dihydroxyacetophenone provide convenient starting nuclei for the design of SHC inhibitors. Derivatives bearing an omega-epoxyfarnesyl moiety or just a plain alkyl chain showed an inhibitory effect on a recombinant SHC from Alicyclobacillus acidocaldarius expressed in Escherichia coli.

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Sigma-Aldrich
2′,6′-二羟基苯乙酮, 97%
Supelco
2′,6′-二羟基苯乙酮, matrix substance for MALDI-MS, ≥99.5%