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Oxidosqualene cyclase inhibitors as antimicrobial agents.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2003 Sep 25; Vol. 46 (20), pp. 4240-3. - Publication Year :
- 2003
-
Abstract
- Small-molecule oxidosqualene cyclase (OSC) inhibitors were found to be effective in assays against cloned OSC-like enzymes from human pathogens. A combinatorial library was prepared and used to identify lead compounds that inhibit the growth of Trypanosoma cruzi, Leishmania mexicana amazonensis, and Pneumocystis carinii in culture. Selectivity for the microorganisms in preference to mammalian cells was observed.
- Subjects :
- 3T3 Cells
Amines chemistry
Animals
Anti-Infective Agents chemistry
Antifungal Agents pharmacology
Antiprotozoal Agents pharmacology
CHO Cells
Combinatorial Chemistry Techniques methods
Cricetinae
Enzyme Inhibitors chemistry
Humans
Inhibitory Concentration 50
Leishmania mexicana drug effects
Leishmania mexicana growth & development
Leishmania mexicana metabolism
Mice
Microbial Sensitivity Tests
Phenols chemistry
Pneumocystis drug effects
Pneumocystis growth & development
Pneumocystis metabolism
Rats
Toxoplasma drug effects
Toxoplasma growth & development
Toxoplasma metabolism
Trypanosoma brucei gambiense drug effects
Trypanosoma brucei gambiense growth & development
Trypanosoma brucei gambiense metabolism
Trypanosoma cruzi drug effects
Trypanosoma cruzi growth & development
Trypanosoma cruzi metabolism
Amines pharmacology
Anti-Infective Agents pharmacology
Enzyme Inhibitors pharmacology
Intramolecular Transferases antagonists & inhibitors
Phenols pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0022-2623
- Volume :
- 46
- Issue :
- 20
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 13678402
- Full Text :
- https://doi.org/10.1021/jm034126t