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Structure-Activity Relationship of the Aminomethylcyclines and the Discovery of Omadacycline
ABSTRACT A series of novel tetracycline derivatives were synthesized with the goal of creating new antibiotics that would be unaffected by the known tetracycline resistance mechanisms. NewExpand
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Structure, DNA minor groove binding, and base pair specificity of alkyl- and aryl-linked bis(amidinobenzimidazoles) and bis(amidinoindoles).
A series of bis(amidinobenzimidazoles) and bis(amidinoindoles) with varied linking chains connecting the aromatic groups and various modifications to the basic amidino groups have been prepared. TheExpand
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Antibacterial agents that inhibit two-component signal transduction systems.
A class of antibacterials has been discovered that inhibits the growth of Gram-positive pathogenic bacteria. RWJ-49815, a representative of a family of hydrophobic tyramines, in addition to being aExpand
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Novel inhibitors of bacterial two-component systems with gram positive antibacterial activity: pharmacophore identification based on the screening hit closantel.
This SAR study has shown that the salicylanilide is the pharmacophore for inhibition of the bacterial two-component system. Hydrophobic substituents improve the potency of inhibitors in this series;Expand
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DNA gyrase inhibitory and antibacterial activity of some flavones (1)
A series of flavones was studied for their DNA-gyrase inhibitory and antibacterial activities, This led to the identification of compounds with potent Escherichia coli DNA-gyrase inhibitory activity,Expand
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Amidino benzimidazole inhibitors of bacterial two-component systems.
Amidino benzimidazoles have been identified as inhibitors of the bacterial KinA/Spo0F two-component system (TCS). Many of these inhibitors exhibit good in vitro antibacterial activity against aExpand
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Structure-activity relationships of analogs of pentamidine against Plasmodium falciparum and Leishmania mexicana amazonensis.
The antiprotozoal compound 1,5-di(4-amidinophenoxy)pentane (pentamidine) and 36 of its analogs were screened for in vitro activity against Leishmania mexicana amazonensis clone 669 C4SExpand
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Testing potential gyrase inhibitors of bacterial DNA gyrase: a comparison of the supercoiling inhibition assay and "cleavable complex" assay.
Inhibitory activity of test compounds against Escherichia coli DNA gyrase in a "cleavable complex" assay, readily observed in vitro at the enzyme level by the artificial addition of a denaturingExpand
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Patents on bacterial tRNA synthetase inhibitors: January 1996 to March 1999
This review focuses on patents published between January 1996 and March 1999 covering bacterial tRNA synthetase inhibitors as antibacterial agents. Nine of the eleven patents issued during thisExpand
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