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Design, synthesis, and biological evaluation of new (2E,6E)-10-(dimethylamino)-3,7-dimethyl-2,6-decadien-1-ol ethers as inhibitors of human and Trypanosoma cruzi oxidosqualene cyclase.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Jan 01; Vol. 17 (1), pp. 220-4. Date of Electronic Publication: 2006 Oct 05. - Publication Year :
- 2007
-
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.
- Subjects :
- Animals
Antiparasitic Agents chemical synthesis
Drug Design
Enzyme Inhibitors chemical synthesis
Humans
Phenyl Ethers chemical synthesis
Phenyl Ethers chemistry
Phenyl Ethers pharmacology
Antiparasitic Agents chemistry
Antiparasitic Agents pharmacology
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Intramolecular Transferases antagonists & inhibitors
Squalene analogs & derivatives
Trypanosoma cruzi enzymology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 17
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 17027267
- Full Text :
- https://doi.org/10.1016/j.bmcl.2006.09.058