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Bioorg Med Chem Lett ; 17(1): 220-4, 2007 Jan 01.
Article in English | MEDLINE | ID: mdl-17027267

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.


Subject(s)
Antiparasitic Agents/chemistry , Antiparasitic Agents/pharmacology , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Intramolecular Transferases/antagonists & inhibitors , Squalene/analogs & derivatives , Trypanosoma cruzi/enzymology , Animals , Antiparasitic Agents/chemical synthesis , Drug Design , Enzyme Inhibitors/chemical synthesis , Humans , Phenyl Ethers/chemical synthesis , Phenyl Ethers/chemistry , Phenyl Ethers/pharmacology
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