Abstract
New dimethylamino truncated squalene ether derivatives containing a different aromatic moiety (phenyl, naphthyl, and biphenyl) or a simple alkyl (n-hexylic) group were synthesized as inhibitors of the oxidosqualene cyclase (OSC) and of the sterol biosynthetic pathway. The activity against human OSC was compared with the activity against the OSCs of pathogenic organisms such as Pneumocystis carinii and Trypanosoma cruzi. The phenyl derivative was the most potent inhibitor of T. cruzi OSC.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antiparasitic Agents / chemical synthesis
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Antiparasitic Agents / chemistry*
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Antiparasitic Agents / pharmacology*
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Drug Design
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacology*
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Humans
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Intramolecular Transferases / antagonists & inhibitors*
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Phenyl Ethers / chemical synthesis
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Phenyl Ethers / chemistry
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Phenyl Ethers / pharmacology
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Squalene / analogs & derivatives*
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Trypanosoma cruzi / enzymology*
Substances
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Antiparasitic Agents
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Enzyme Inhibitors
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Phenyl Ethers
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Squalene
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Intramolecular Transferases
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lanosterol synthase