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Abstract
Thirteen structural analogs of two initial intermediates of the L-alpha-aminoadipate pathway of L-lysine biosynthesis in fungi have been designed and synthesized, including fluoro- and epoxy-derivatives of homoaconitate and homoisocitrate. Some of the obtainedcompounds exhibited at milimolar range moderate enzyme inhibitory properties against homoaconitase and/or homoisocitrate dehydrogenase of Candida albicans. The structural basis for homoisocitrate dehydrogenase inhibition was revealed by molecular modeling ofthe enzyme-inhibitor complex. On the other hand, the trimethyl ester forms of some of the novel compounds exhibited antifungal effects. The highest antifungal activity was found for trimethyl trans-homoaconitate, which inhibited growth of some human pathogenicyeasts with minimal inhibitory concentration (MIC) values of 16-32 mcg/mL.
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- Category:
- Articles
- Type:
- artykuł w czasopiśmie wyróżnionym w JCR
- Published in:
-
MOLECULES
no. 17,
pages 14022 - 14036,
ISSN: 1420-3049 - Language:
- English
- Publication year:
- 2012
- Bibliographic description:
- Milewska M. J., Prokop M., Gabriel I., Wojciechowski M., Milewski S.: Antifungal Activity of Homoaconitate and Homoisocitrate Analogs// MOLECULES. -Vol. 17, iss. iss. 12 (2012), s.14022-14036
- Verified by:
- Gdańsk University of Technology
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