ampicillin-sodium and Staphylococcal-Infections

ampicillin-sodium has been researched along with Staphylococcal-Infections* in 2 studies

Other Studies

2 other study(ies) available for ampicillin-sodium and Staphylococcal-Infections

Article	Year
Synthesis, in vitro antibacterial activities of a series of 3-N-substituted canthin-6-ones. Bioorganic & medicinal chemistry letters, 2016, Jan-15, Volume: 26, Issue:2 An improved synthetic route of canthin-6-one was accomplished. To further enhance the antibacterial potency and improve water solubility, a series of 3-N-alkylated and 3-N-benzylated canthin-6-ones were designed and synthesized, and their in vitro antibacterial activities were evaluated. A clear structure-activity relationship with peak minimal inhibitory concentration (MIC) values of 0.98 (μg·mL(-)(1)) was investigated. Particularly, compounds 6i-r and 6t were found to be the most potent compounds with minimal inhibitory concentration (MIC) values lower than 1.95 (μg·mL(-)(1)) against Staphylococcus aureus. Topics: Alkylation; Anti-Bacterial Agents; Carbolines; Humans; Indole Alkaloids; Microbial Sensitivity Tests; Staphylococcal Infections; Staphylococcus aureus; Structure-Activity Relationship	2016
A bactericidal guanidinomethyl biaryl that alters the dynamics of bacterial FtsZ polymerization. Journal of medicinal chemistry, 2012, Nov-26, Volume: 55, Issue:22 The prevalence of multidrug resistance among clinically significant bacterial pathogens underscores a critical need for the development of new classes of antibiotics with novel mechanisms of action. Here we describe the synthesis and evaluation of a guanidinomethyl biaryl compound {1-((4'-(tert-butyl)-[1,1'-biphenyl]-3-yl)methyl)guanidine} that targets the bacterial cell division protein FtsZ. In vitro studies with various bacterial FtsZ proteins reveal that the compound alters the dynamics of FtsZ self-polymerization via a stimulatory mechanism, while minimally impacting the polymerization of tubulin, the closest mammalian homologue of FtsZ. The FtsZ binding site of the compound is identified through a combination of computational and mutational approaches. The compound exhibits a broad spectrum of bactericidal activity, including activity against the multidrug-resistant pathogens methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE), while also exhibiting a minimal potential to induce resistance. Taken together, our results highlight the compound as a promising new FtsZ-targeting bactericidal agent. Topics: Anti-Bacterial Agents; Bacterial Proteins; Biphenyl Compounds; Cytoskeletal Proteins; Drug Resistance, Multiple; Enterococcus; Guanidines; Methicillin-Resistant Staphylococcus aureus; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Polymerization; Staphylococcal Infections; Staphylococcus aureus; Structure-Activity Relationship; Vancomycin Resistance	2012

Article

Year

Synthesis, in vitro antibacterial activities of a series of 3-N-substituted canthin-6-ones.

Bioorganic & medicinal chemistry letters, 2016, Jan-15, Volume: 26, Issue:2

An improved synthetic route of canthin-6-one was accomplished. To further enhance the antibacterial potency and improve water solubility, a series of 3-N-alkylated and 3-N-benzylated canthin-6-ones were designed and synthesized, and their in vitro antibacterial activities were evaluated. A clear structure-activity relationship with peak minimal inhibitory concentration (MIC) values of 0.98 (μg·mL(-)(1)) was investigated. Particularly, compounds 6i-r and 6t were found to be the most potent compounds with minimal inhibitory concentration (MIC) values lower than 1.95 (μg·mL(-)(1)) against Staphylococcus aureus.

Topics: Alkylation; Anti-Bacterial Agents; Carbolines; Humans; Indole Alkaloids; Microbial Sensitivity Tests; Staphylococcal Infections; Staphylococcus aureus; Structure-Activity Relationship

2016

A bactericidal guanidinomethyl biaryl that alters the dynamics of bacterial FtsZ polymerization.

Journal of medicinal chemistry, 2012, Nov-26, Volume: 55, Issue:22

The prevalence of multidrug resistance among clinically significant bacterial pathogens underscores a critical need for the development of new classes of antibiotics with novel mechanisms of action. Here we describe the synthesis and evaluation of a guanidinomethyl biaryl compound {1-((4'-(tert-butyl)-[1,1'-biphenyl]-3-yl)methyl)guanidine} that targets the bacterial cell division protein FtsZ. In vitro studies with various bacterial FtsZ proteins reveal that the compound alters the dynamics of FtsZ self-polymerization via a stimulatory mechanism, while minimally impacting the polymerization of tubulin, the closest mammalian homologue of FtsZ. The FtsZ binding site of the compound is identified through a combination of computational and mutational approaches. The compound exhibits a broad spectrum of bactericidal activity, including activity against the multidrug-resistant pathogens methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE), while also exhibiting a minimal potential to induce resistance. Taken together, our results highlight the compound as a promising new FtsZ-targeting bactericidal agent.

Topics: Anti-Bacterial Agents; Bacterial Proteins; Biphenyl Compounds; Cytoskeletal Proteins; Drug Resistance, Multiple; Enterococcus; Guanidines; Methicillin-Resistant Staphylococcus aureus; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Polymerization; Staphylococcal Infections; Staphylococcus aureus; Structure-Activity Relationship; Vancomycin Resistance

2012