Abstract
A series of 25 compounds, some of which previously were described as inhibitors of human liver microsomal oxidosqualene cyclase (OSC), were tested as inhibitors of Saccharomyces cerevisiae, Trypanosoma cruzi, Pneumocystis carinii and Arabidopsis thaliana OSCs expressed in an OSC-defective strain of S. cerevisiae. The screening identified three derivatives particularly promising for the development of novel anti-Trypanosoma agents and eight derivatives for the development of novel anti-Pneumocystis agents.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Antiparasitic Agents / chemical synthesis*
-
Antiparasitic Agents / pharmacology*
-
Arabidopsis / enzymology*
-
Chemistry, Pharmaceutical / methods*
-
Chromatography, Thin Layer
-
Drug Design
-
Humans
-
Intramolecular Transferases / chemistry*
-
Intramolecular Transferases / metabolism
-
Microsomes, Liver / metabolism
-
Models, Chemical
-
Pneumocystis carinii / enzymology*
-
Saccharomyces cerevisiae / enzymology*
-
Sterols / chemistry
-
Trypanosoma cruzi / enzymology*
Substances
-
Antiparasitic Agents
-
Sterols
-
Intramolecular Transferases
-
lanosterol synthase