scholarly journals The effect of acylated polyamine derivatives on polyamine uptake mechanism, cell growth, and polyamine pools in Escherichia coli, and the pursuit of structure/activity relationships

1998 ◽  
Vol 251 (3) ◽  
pp. 998-1004 ◽  
Author(s):  
Panagiotis Karahalios ◽  
Petros Mamos ◽  
Dimitrios H. Vynios ◽  
Dionissios Papaioannou ◽  
Dimitrios L. Kalpaxis
Keyword(s):  
Escherichia Coli ◽  
Cell Growth ◽  
Uptake Mechanism ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Polyamine Uptake ◽  
Polyamine Derivatives

scholarly journals Structure-activity relationships of puromycin analogues on Escherichia coli polysomes

FEBS Letters ◽  
1974 ◽  
Vol 40 (1) ◽  
pp. 124-126 ◽  
Author(s):  
Elio F. Vanin ◽  
Philip Greenwell ◽  
Robert H. Symons
Keyword(s):  
Escherichia Coli ◽  
Structure Activity Relationships ◽  
Structure Activity

scholarly journals Structure-activity relationships of 3-substituted-5,5- diphenylhydantoins as potential antiproliferative and antimicrobial agents

2011 ◽  
Vol 76 (12) ◽  
pp. 1597-1606 ◽  
Author(s):  
Nemanja Trisovic ◽  
Bojan Bozic ◽  
Ana Obradovic ◽  
Olgica Stefanovic ◽  
Snezana Markovic ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Agents ◽  
Human Colon ◽  
Antibacterial Activities ◽  
E Coli ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Almost All

A series of twelve 3-substituted-5,5-diphenylhydantoins was synthesized, including some whose anticonvulsant activities have already been reported in the literature. Their antiproliferative activities against HCT-116 human colon carcinoma cells were evaluated to determine structure-activity relationships. Almost all of the compounds exhibited statistically significant antiproliferative effects at a concentration of 100 ?M, while the derivative bearing a benzyl group was active even at lower concentrations. Moreover, their in vitro antibacterial activities against Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923 and clinical isolates of Escherichia coli, Proteus mirabilis, Pseudomonas aeruginosa, Enterococcus faecalis and Staphylococcus aureus were evaluated. Only the 3-iso-propyl and 3-benzyl derivatives showed weak antibacterial activities against the Gram-positive bacterium E. faecalis and the Gram-negative bacteria E. coli ATCC 25922 and E. coli.

scholarly journals Fluorescence Polarization Method To Characterize Macrolide-Ribosome Interactions

2005 ◽  
Vol 49 (8) ◽  
pp. 3367-3372 ◽  
Author(s):  
Kang Yan ◽  
Eric Hunt ◽  
John Berge ◽  
Earl May ◽  
Robert A. Copeland ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Binding Sites ◽  
Fluorescence Polarization ◽  
Binding Assay ◽  
Dissociation Constants ◽  
Polarization Method ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Fluorescence Polarization Assay

ABSTRACT A fluorescence polarization assay is described that measures the binding of fluorescently labeled erythromycin to 70S ribosomes from Escherichia coli and the displacement of the erythromycin from these ribosomes. The assay has been validated with several macrolide derivatives and other known antibiotics. We demonstrate that this assay is suitable for determining the dissociation constants of novel compounds that have binding sites overlapping those of macrolides. This homogeneous binding assay provides a valuable tool for defining structure-activity relationships among compounds during the discovery and development of new ribosome-targeting drugs.

Structure-activity relationships of sparsomycin and its analogs. Inhibition of peptide bond formation in cell-free systems and of L1210 and bacterial cell growth

1987 ◽  
Vol 30 (2) ◽  
pp. 325-333 ◽  
Author(s):  
Leon A. G. M. Van den Broek ◽  
Rob M. J. Liskamp ◽  
J. Hans Colstee ◽  
Peter Lelieveld ◽  
Miguel Remacha ◽  
...  
Keyword(s):  
Cell Growth ◽  
Bacterial Cell ◽  
Bond Formation ◽  
Peptide Bond ◽  
Peptide Bond Formation ◽  
Structure Activity Relationships ◽  
Structure Activity
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