- Substituted pyrazolo-piperazines as casein kinase 1 δ/ε inhibitors
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The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.
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Page/Page column 341; 342
(2016/03/19)
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- Fungicidal amides
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Compounds of Formula I are disclosed which are useful as fungicides wherein R1is hydrogen; halogen; C1-C2alkoxy; C1-C2haloalkoxy; cyano; or C1-C2alkyl optionally substituted with halogen, C1-C2alkoxy or cyano; R2is hydrogen; halogen; or C1-C4alkyl optionally substituted with halogen, C1-C2alkoxy or cyano; R3is hydrogen; halogen; C1-C4alkoxy; C1-C4haloalkoxy; or C1-C4alkyl optionally substituted with halogen, C1-C2alkoxy or cyano; or R2and R3can be taken together as —CH2CH2—; R4is C1-C2alkyl; R5is R6, CH(R8)OR6, CH(R8)CH(R7)R6or C(R8)═C(R7)R6; and R6, R7and R8are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula I.
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- Cyclobutane carboxamide inhibitors of fungal melanin: Biosynthesis and their evaluation as fungicides
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A new fungicide lead has been identified by enzyme screening of a focused combinatorial library. The lead compound 4 Inhibitors of scytalone dehydratase (SD)., a potent inhibitor of scytalone dehydratase (SD), exhibits fungicidal activity upon foliar application but does not show systemic activity. The X-ray crystal structure of the enzyme-inhibitor complex and an appreciation for the relationship between physical properties and systemic activity enabled us to rapidly improve upon this initial lead. The geminal halogen-methyl group combination was found to be optimal for interaction with the bounding serine and asparagine side-chain residues. Replacement of CF3 with methyl was a key discovery, giving inhibitors with slightly diminished enzyme inhibition potency while significantly increasing systemic activity. Amides prepared from amines with 2,4-dichloro substitution on the phenyl ring gave the most potent enzyme inhibitors. Two compounds from this series showed systemic activity comparable to the commercial standard and were selected for outdoor testing in flooded plots which simulate rice paddies. (C) 2000 Elsevier Science Ltd.
- Jennings, Lee D.,Rayner, Dennis R.,Jordan, Douglas B.,Okonya, John F.,Basarab, Gregory S.,Amorose, Denise K.,Anaclerio, Beth M.,Lee, John K.,Schwartz, Rand S.,Whitmore, Kari Ann
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p. 897 - 907
(2007/10/03)
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