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Using an X-ray crystallography/structure-based design approach, the benzomorpholinone series was further optimised, increasing activity against T. brucei NMT by >1000-fold.
If not, could it be that the sequence context of R1-11 promotes improvements towards 2-phenoxyethanol because of some specific position on the neutral network that elevate the chances of increasing activity against 2-phenoxyethanol?
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First-generation cephalosporins (cephalexin, cefadroxil) are predominantly active against Gram-positive bacteria, and successive generations have increased activity against Gram-negative bacteria (cefoperazone) [1 3].
Among the LigI-selective inhibitors, L82-G17 exhincreasedcreactivityivity against and selectivity for LigI compared with L82.
Both analogues showed an increased activity against HL-60 cells with 17- and 185-fold higher potency than -muricatacin.
The third-generation cephalosporins (ceftriaxone, cefixime, and ceftazidime) have increased activity against the gram-negative organisms compared with the second-generation agents.
Generally, introduction of hydrophobic moieties at the N-terminus resulted in analogues with remarkably increased activity against multidrug-resistant Staphylococcus aureus and Enterococcus faecium.
Herein, using a cell based assay that we developed, we identify two new aminoadamantyl derivatives that show increased activity against otherwise resistant M2 variants.
The in vitro cytotoxicity and cell uptake studies in human breast carcinoma cell line (MCF-7 and MDA-MB-231) as well as in healthy human skin fibroblasts (DSF) show uptake of the intact complexes by cancer cells and increased activity against cancer cell lines.
Compared with ciprofloxacin, levofloxacin has an increased activity against gram-positive bacteria.
MGAH22 demonstrates increased activity against HER2-expressing tumors in mice transgenic for human CD16A-158F.
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