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A new potent inhibitor of fungal melanin biosynthesis identified through combinatorial chemistry
A new fungicide lead has been identified by in vitro screening of a focused combinatorial library. Amides (768) were synthesized in pools of four and assayed as inhibitors of scytalone dehydratase. Deconvolution of one of the most active pools led to the discovery of a potent inhibitor of the enzyme...
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| Published in: | Bioorganic & medicinal chemistry letters 1999-09, Vol.9 (17), p.2509-2514 |
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| Main Authors: | , , , , |
| Format: | Article |
| Language: | English |
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| cited_by | cdi_FETCH-LOGICAL-c390t-bbcb9645b9ad4212b281b54ded6bda4c5cf593cc8713e3bc65e657d33aa1576e3 |
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| cites | cdi_FETCH-LOGICAL-c390t-bbcb9645b9ad4212b281b54ded6bda4c5cf593cc8713e3bc65e657d33aa1576e3 |
| container_end_page | 2514 |
| container_issue | 17 |
| container_start_page | 2509 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 9 |
| creator | Jennings, Lee D. Wawrzak, Zdzislaw Amorose, Denise Schwartz, Rand S. Jordan, Douglas B. |
| description | A new fungicide lead has been identified by in vitro screening of a focused combinatorial library. Amides (768) were synthesized in pools of four and assayed as inhibitors of scytalone dehydratase. Deconvolution of one of the most active pools led to the discovery of a potent inhibitor of the enzyme
3b (K
i = 26 pM), which has fungicidal properties. |
| doi_str_mv | 10.1016/S0960-894X(99)00424-2 |
| format | article |
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| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 1999-09, Vol.9 (17), p.2509-2514 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | ScienceDirect Freedom Collection |
| subjects | Antibiotics. Antiinfectious agents. Antiparasitic agents Antifungal agents Biological and medical sciences Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Hydro-Lyases - antagonists & inhibitors Hydro-Lyases - chemistry Hydro-Lyases - metabolism Magnaporthe - drug effects Magnaporthe - enzymology Magnaporthe - metabolism Medical sciences Melanins - antagonists & inhibitors Melanins - biosynthesis Models, Molecular Pharmacology. Drug treatments |
| title | A new potent inhibitor of fungal melanin biosynthesis identified through combinatorial chemistry |
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