Abstract
CGP-291 is an investigational antiprotozoal agent with unknown metabolism. Microbial systems were utilized, as a model of mammalian metabolism, to predict the oxidative metabolic pathway of this nitroimidazole. Large-scale fermentation of CGP-291 with Beauvaria bassiana produced two major metabolites, IV and V. Structures of both were elucidated by comparing spectral data of metabolites to that of the starting material. The presence of two minor monohydroxylated metabolites was verified using LC-MS.
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REFERENCES
A. O. Ilvespää and R. Jarumilinta. Indian J. Chem. 21B:923–927 (1982).
Drugs Future 8:581–582 (1983).
J. W. Faigle, D. M. Blair, V. de V. Clarke, L. A. G. Davidson, D. C. Dukes, and H. Keberle. Ann. Trop. Med. Parasitol. 64:373–382 (1970).
J. W. Faigle, A. D. Coutinho, H. Keberle, and F. Trindade Barretto. Ann. Trop. Med. Parasitol. 64:383–392 (1970).
J. W. Tracy, B. A. Catto, and L. T. Webster, Jr. Mol. Pharmacol. 24:291–299 (1983).
J. W. Tracy, E. H. Fairchild, S. V. Lucas, and L. T. Webster, Jr. Mol. Pharmacol. 18:313–319 (1980).
J. L. Blumer, R. F. Novak, S. V. Lucas, J. M. Simpson, and L. T. Webster, Jr. Mol. Pharmacol. 16:1019–1030 (1979).
P. J. Davis, S.-K. Yang, and R. V. Smith. Xenobiotica 15:1001–1010 (1985).
A. M. Clark, J. D. McChesney, and C. D. Hufford. Med. Res. Rev. 5:231–253 (1985).
A. M. Clark, C. D. Hufford, and J. D. McChesney. Antimicrob. Agents Chemother. 19:337–341 (1981).
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Jürgens, T.M., Clark, A.M. The Metabolism of CGP-291: The Use of Microorganisms as Models of Mammalian Metabolism. Pharm Res 7, 742–745 (1990). https://doi.org/10.1023/A:1015871723330
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DOI: https://doi.org/10.1023/A:1015871723330