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Oxidosqualene cyclase inhibitors as antimicrobial agents.
| Title | Oxidosqualene cyclase inhibitors as antimicrobial agents. |
| Publication Type | Journal Article |
| Year of Publication | 2003 |
| Authors | Hinshaw, JC, Suh, D-Y, Garnier, P, Buckner, FS, Eastman, RT, Matsuda, SPT, Joubert, BM, Coppens, I, Joiner, KA, Merali, S, Nash, TE, Prestwich, GD |
| Journal | J Med Chem |
| Volume | 46 |
| Issue | 20 |
| Pagination | 4240-3 |
| Date Published | 2003 Sep 25 |
| ISSN | 0022-2623 |
| Keywords | 3T3 Cells, Amines, Animals, Anti-Infective Agents, Antifungal Agents, Antiprotozoal Agents, CHO Cells, Combinatorial Chemistry Techniques, Cricetinae, Enzyme Inhibitors, Humans, Inhibitory Concentration 50, Intramolecular Transferases, Leishmania mexicana, Mice, Microbial Sensitivity Tests, Phenols, Pneumocystis, Rats, Toxoplasma, Trypanosoma brucei gambiense, Trypanosoma cruzi |
| 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. |
| DOI | 10.1021/jm034126t |
| Alternate Journal | J. Med. Chem. |
| PubMed ID | 13678402 |
