Enzyme inhibitory

More recently, screening efforts at Novartis have identified a hydroxamic acid containing a benzothiazinone ring system (32) [108]. This inhibitor is very potent versus S. aureus Ni -PDF (<5nM) and displays good selectivity versus matrix metalloprotease-2 (MMP-2) and MMP-13. Unfortunately (32), and all other analogues prepared, such as carbon isosteres (33), sulfones (34), N-substituted analogues (35) and N-formyl-N-hydroxylamines (36), lacked appreciable antibacterial activity in spite of their potent enzyme inhibitory activity. Further studies performed by Novartis suggest that these molecules are unable to penetrate the outer cell membrane of E. coli, and may bind to the cell membrane of S. aureus [108]. 

Microtiter plates HRP/H202/luminol AP/dioxetanes Firefly luciferin/luciferase Bacterial luciferin/luciferase Detection of enzymes and metabolites by direct or coupled enzyme reactions Determination of antioxidant and enzyme inhibitory activities Immunoassay... 

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Second- and Third-Generation Antidepressants and Cytochrome (CYP) P450 Enzyme Inhibitory Potential... 

The results of enzymatic and antibacterial assays demonstrated that compound 165 (as a racemic mixture) exhibits activities similar to those of the parent oxazoline L-159,692 [103]. In order to identify the enantioselectiv-ity of this compound, the corresponding R and S enantiomers were separately synthesized from (R)- or (S)-3-(4-methoxyphenyl)-5-hydroxymethyl-4,5-dihydroisoxazole (166) according to the method of Ukaji et al. [107,108] and tested for LpxC inhibitory and antibacterial activities [103]. Interestingly, only the S enantiomer of 166 exhibited strong enzyme inhibitory and antibacterial activity, while the R enantiomer of L-159,692 was the active component. The enantiomeric synthesis of compound 165 is depicted in Scheme 33. 

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