Conjugated methyl sulfide and phenyl sulfide derivatives of oxidosqualene as inhibitors of oxidosqualene and squalene-hopene cyclases |
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Authors: | Flavio?Rocco Simonetta?Oliaro?Bosso Franca?Viola Paola?Milla Giorgio?Roma Giancarlo?Grossi Email author" target="_blank">Maurizio?CerutiEmail author |
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Affiliation: | (1) Dipartimento di Scienze Farmaceutiche, Università degli Studi di Genova, 16132 Genova, Italy;(2) Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Via Pietro Giuria 9, 10125 Torino, Italy |
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Abstract: | Various (1E,3E)- and (1Z,3E)-conjugated methylthio derivatives of oxidosqualene (OS) and conjugated and non-conjugated phenylthio derivatives of OS were
obtained. These compounds, designed as inhibitors of pig liver and Saccharomyces cerevisiae 2,3-oxidosqualene-lanosterol cyclases (OSC) (EC 5.4.99.7) and of Alicyclobacillus acidocaldarius squalenehopene cyclase (SHC) (EC 5.4.99.-), contain the reactive function adjacent to carbons involved in the formation of
the third and the fourth cycle during OS cyclization. All the new compounds are inhibitors of OSC and SHC, with various degrees
of selectivity. The conjugated methylthio derivatives behaved as potent inhibitors of S. cerevisiae OSC, whereas most of the phenylthio derivatives were especially active toward SHC. |
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