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Compounds lacking the double bond were found to be inactive (e.g. 3-phenylpropionaldehyde and 4-phenyl-2-butanone) (Fig. 1; Table 1).
Craven and others have previously assigned the W7 analogue J8 through the use of analogous compounds lacking the problematically high symmetry (13).
For example, indole is associated with an increase in biological activity in the Chembridge library assays among compounds lacking the substructures shown at nodes 1, 3, 5, 8 and 11.
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However, these compounds lacked the selectivity of other serine proteases in the coagulation cascade, especially thrombin.
However, the synthesized compounds lack the activities against HIV-1 double mutant (RES056) and HIV-2 (ROD).
These non-peptidic compounds lack the classical zinc-binding groups (ZBG) present in most of the APN inhibitors.
The antifungal activity was labile to modification of the enol ether functionality and almost all of the modified compounds lacked the activity except for the analogue with an introduction of a methylthio group at the C-6 position, which retained a modest antifungal potency against Cryptococcus neoformans.
Differentiated macrophages were pretreated for 1 h with 0.2 μM solutions of the tested complexes, prednisone or CuSO4 · 5 H2O dissolved in DMSO (the final DMSO concentration was 0.1%) and with 0.1% DMSO solution itself (the experimental group called vehicle); the given concentrations of the tested compounds lack the cytotoxic effect.
Early medicinal chemistry efforts revealed that these compounds lacked the characteristics desired for further development.
Several compounds lacked the inhalation data requiring oral toxicity factors to be used to estimate the index.
Not only do the lead compounds lack the phosphates, but they are also modified at the amino position, which could affect Asp binding and increase steric hindrance.
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