63472-21-9Relevant articles and documents
2-AMINO-1,3,4-THIADIAZINE AND 2-AMINO-1,3,4-OXADIAZINE BASED ANTIFUNGAL AGENTS
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, (2017/02/09)
The invention provides a compound which is a diazine of formula (I) or a tautomer thereof, or a pharmaceutically acceptable salt thereof, for use as an antifungal agent: (I) wherein X, N', C', A and E are as defined herein. The invention also provides a compound of Formula (I) as defined herein.
Discovery of potent nonpeptide inhibitors of stromelysin using SAR by NMR
Hajduk,Sheppard,Nettesheim,Olejniczak,Shuker,Meadows,Steinman,Carrera Jr.,Marcotte,Severin,Walter,Smith,Gubbins,Simmer,Holzman,Morgan,Davidsen,Summers,Fesik
, p. 5818 - 5827 (2007/10/03)
With the use of an NMR-based method, potent (IC50 25 nM) nonpeptide inhibitors of the matrix metalloproteinase stromelysin (MMP-3) were discovered. The method, called SAR by NMR (for structure-activity relationships by nuclear magnetic resonance), involves the identification, optimization, and linking of compounds that bind to proximal sites on a protein. Using this technique, two ligands that bind weakly to stromelysin (acetohydroxamic acid, K(D) = 17 mM; 3-(cyanomethyl)-4'-hydroxybiphenyl, K(D) = 0.02 mM) were identified. On the basis of NMR-derived structural information, the two fragments were connected to produce a 15 nM inhibitor of this enzyme. This compound was rapidly discovered (less than 6 months) and required only a minimal amount of chemical synthesis. These studies indicate that the SAR by NMR method can be effectively applied to enzymes to yield potent lead inhibitors-an important part of the drug discovery process.
Substituted benzopyran and tetrahydronaphthalene compounds useful for safening herbicides in crops
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, (2008/06/13)
There is provided a method for safening herbicides in crop plants by using substituted benzopyran or tetrahydronaphthalene compounds of formula I STR1 Further provided are compounds of formula II and compositions comprising a herbicide and an antidotally