scholarly journals In vitro and in vivo antibacterial activities of FK037, a novel parenteral broad-spectrum cephalosporin.

1993 ◽  
Vol 37 (2) ◽  
pp. 301-307 ◽  
Author(s):  
K P Fu ◽  
B D Foleno ◽  
S C Lafredo ◽  
J M LoCoco ◽  
D M Isaacson
Keyword(s):  
Broad Spectrum ◽  
Antibacterial Activities

scholarly journals SCE-963, a New Broad-Spectrum Cephalosporin: In Vitro and In Vivo Antibacterial Activities

1978 ◽  
Vol 14 (4) ◽  
pp. 557-568 ◽  
Author(s):  
K. Tsuchiya ◽  
M. Kida ◽  
M. Kondo ◽  
H. Ono ◽  
M. Takeuchi ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Antibacterial Activities

scholarly journals Cefmenoxime (SCE-1365), a novel broad-spectrum cephalosporin: in vitro and in vivo antibacterial activities.

1981 ◽  
Vol 19 (1) ◽  
pp. 56-65 ◽  
Author(s):  
K Tsuchiya ◽  
M Kondo ◽  
M Kida ◽  
M Nakao ◽  
T Iwahi ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Antibacterial Activities

In Vitro and In Vivo Antibacterial Activities of Broad Spectrum Quinolones against Clinical Bacterial Isolates

Drugs ◽  
1995 ◽  
Vol 49 (Supplement 2) ◽  
pp. 219-221
Author(s):  
T. Matsumoto ◽  
K. Tateda ◽  
Y. Ishii ◽  
A. Ohno ◽  
S. Miyazaki ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Antibacterial Activities ◽  
Bacterial Isolates

scholarly journals In vitro and in vivo antibacterial activities of GV129606, a new broad-spectrum trinem.

1997 ◽  
Vol 41 (12) ◽  
pp. 2742-2748 ◽  
Author(s):  
E Di Modugno ◽  
R Broggio ◽  
I Erbetti ◽  
J Lowther
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Broad Spectrum ◽  
Antibacterial Activities ◽  
Beta Lactam ◽  
Beta Lactamases ◽  
Streptococcus Sanguis ◽  
Spectrum Activity ◽  
Providencia Stuartii

GV129606 is a new parenteral trinem antibiotic belonging to the beta-lactam class. It combines broad-spectrum activity (against gram-negative and -positive bacteria, aerobes and anaerobes), with high potency and resistance to beta-lactamases. Comparative in vitro and in vivo antibacterial activities were determined for GV129606 against more than 400 recent clinical isolates (aerobes, including beta-lactamase producers, and anaerobes), using representative antibacterial agents (meropenem, piperacillin, ceftazidime, cefpirome, ciprofloxacin, and gentamicin for aerobes and metronidazole, cefoxitin, piperacillin, and clindamycin for anaerobes). Against methicillin-susceptible staphylococci and streptococci, GV129606 and meropenem were the most active of the drugs tested. GV129606 showed an MIC for 90% of strains tested (MIC90) ranging from < or =0.015 to 0.06 microg/ml against methicillin-susceptible staphylococci and Streptococcus sanguis, Streptococcus pyogenes, and Streptococcus agalactiae. Against penicillin-susceptible and -resistant Streptococcus pneumoniae isolates, GV129606, meropenem, and cefpirome showed MIC90s of < or =0.015 and 1 microg/ml, respectively. Meropenem was the most active compound against members of the family Enterobacteriaceae with MIC90s of < or =0.5 microg/ml. Against these species, GV129606 possessed activity superior to those of piperacillin, ceftazidime, cefpirome, and gentamicin, with MIC90s of < or =8 microg/ml, but its activity was two- to sixfold less than that of ciprofloxacin (with the exception of Proteus rettgeri and Providencia stuartii). Haemophilus spp., Moraxella catarrhalis, Neisseria gonorrhoeae, and Pseudomonas aeruginosa were also included in the spectrum of GV129606. GV129606 showed good antianaerobe activity, similar to metronidazole. It was stable against all clinically relevant beta-lactamases (similar to meropenem). The in vitro activity was confirmed in vivo against septicemia infections induced in mice by selected gram-positive and -negative bacteria with 50% effective doses (ED50s) of < or =0.05 and < or =0.5 mg/kg of body weight/dose, respectively. GV129606 was as effective as meropenem against septicemia in mice caused by ceftazidime-resistant Pseudomonas aeruginosa, exhibiting an ED50 of 0.33 mg/kg/dose.

scholarly journals In vitro and in vivo antibacterial activities of AT-4140, a new broad-spectrum quinolone.

1989 ◽  
Vol 33 (8) ◽  
pp. 1167-1173 ◽  
Author(s):  
S Nakamura ◽  
A Minami ◽  
K Nakata ◽  
N Kurobe ◽  
K Kouno ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Antibacterial Activities

scholarly journals Antibacterial activities in vitro and in vivo and pharmacokinetics of cefquinome (HR 111V), a new broad-spectrum cephalosporin.

1991 ◽  
Vol 35 (1) ◽  
pp. 14-19 ◽  
Author(s):  
M Limbert ◽  
D Isert ◽  
N Klesel ◽  
A Markus ◽  
K Seeger ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Antibacterial Activities

In Vitro and In Vivo Antibacterial Activities of CFC-222, a Novel Broad Spectrum Fluoroquinolone

Drugs ◽  
1995 ◽  
Vol 49 (Supplement 2) ◽  
pp. 240-242 ◽  
Author(s):  
K.H. Park ◽  
I.H. Cho ◽  
J.M. Lee ◽  
J.A. Kang ◽  
Y.G. Kim ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Antibacterial Activities

Design, Synthesis, and Pharmacokinetic Evaluation of O-Carbamoyl Tizoxanide Prodrugs

2020 ◽  
Vol 16 ◽  
Author(s):  
Xi He ◽  
Wenjun Hu ◽  
Fanhua Meng ◽  
Xingzhou Li
Keyword(s):  
Plasma Concentration ◽  
Broad Spectrum ◽  
Plasma Concentrations ◽  
Antiviral Drug ◽  
Systemic Exposure ◽  
Pharmacokinetic Profile ◽  
Hydroxyl Group ◽  
First Pass

Background: The broad-spectrum antiparasitic drug nitazoxanide (N) has been repositioned as a broad-spectrum antiviral drug. Nitazoxanide’s in vivo antiviral activities are mainly attributed to its metabolitetizoxanide, the deacetylation product of nitazoxanide. In reference to the pharmacokinetic profile of nitazoxanide, we proposed the hypotheses that the low plasma concentrations and the low system exposure of tizoxanide after dosing with nitazoxanide result from significant first pass effects in the liver. It was thought that this may be due to the unstable acyloxy bond of nitazoxanide. Objective: Tizoxanide prodrugs, with the more stable formamyl substituent attached to the hydroxyl group rather than the acetyl group of nitazoxanide, were designed with the thought that they might be more stable in plasma. It was anticipated that these prodrugs might be less affected by the first pass effect, which would improve plasma concentrations and system exposure of tizoxanide. Method: These O-carbamoyl tizoxanide prodrugs were synthesized and evaluated in a mouse model for pharmacokinetic (PK) properties and in an in vitro model for plasma stabilities. Results: The results indicated that the plasma concentration and the systemic exposure of tizoxanide (T) after oral administration of O-carbamoyl tizoxanide prodrugs were much greater than that produced by equimolar dosage of nitazoxanide. It was also found that the plasma concentration and the systemic exposure of tizoxanide glucuronide (TG) were much lower than that produced by nitazoxanide. Conclusion: Further analysis showed that the suitable plasma stability of O-carbamoyl tizoxanide prodrugs is the key factor in maximizing the plasma concentration and the systemic exposure of the active ingredient tizoxanide.

scholarly journals Antibacterial Mechanisms and Efficacy of Sarecycline in Animal Models of Infection and Inflammation

Antibiotics ◽  
2021 ◽  
Vol 10 (4) ◽  
pp. 439
Author(s):  
Christopher G. Bunick ◽  
Jonette Keri ◽  
S. Ken Tanaka ◽  
Nika Furey ◽  
Giovanni Damiani ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Bacterial Resistance ◽  
Antibiotic Use ◽  
In Vivo Studies ◽  
Infection Model ◽  
Severe Acne ◽  
Rat Paw Edema ◽  
Infection And Inflammation

Prolonged broad-spectrum antibiotic use is more likely to induce bacterial resistance and dysbiosis of skin and gut microflora. First and second-generation tetracycline-class antibiotics have similar broad-spectrum antibacterial activity. Targeted tetracycline-class antibiotics are needed to limit antimicrobial resistance and improve patient outcomes. Sarecycline is a narrow-spectrum, third-generation tetracycline-class antibiotic Food and Drug Administration (FDA)-approved for treating moderate-to-severe acne. In vitro studies demonstrated activity against clinically relevant Gram-positive bacteria but reduced activity against Gram-negative bacteria. Recent studies have provided insight into how the structure of sarecycline, with a unique C7 moiety, interacts with bacterial ribosomes to block translation and prevent antibiotic resistance. Sarecycline reduces Staphylococcus aureus DNA and protein synthesis with limited effects on RNA, lipid, and bacterial wall synthesis. In agreement with in vitro data, sarecycline demonstrated narrower-spectrum in vivo activity in murine models of infection, exhibiting activity against S. aureus, but reduced efficacy against Escherichia coli compared to doxycycline and minocycline. In a murine neutropenic thigh wound infection model, sarecycline was as effective as doxycycline against S. aureus. The anti-inflammatory activity of sarecycline was comparable to doxycycline and minocycline in a rat paw edema model. Here, we review the antibacterial mechanisms of sarecycline and report results of in vivo studies of infection and inflammation.

scholarly journals In Vitro and In Vivo Antibacterial Activities of DW-224a, a New Fluoronaphthyridone

2006 ◽  
Vol 50 (6) ◽  
pp. 2261-2264 ◽  
Author(s):  
Hee-Soo Park ◽  
Hyun-Joo Kim ◽  
Min-Jung Seol ◽  
Dong-Rack Choi ◽  
Eung-Chil Choi ◽  
...  
Keyword(s):  
Antibacterial Activities ◽  
The Other ◽  
Vitro Activity ◽  
Gram Negative Bacteria ◽  
In Vitro Activity ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria

ABSTRACT DW-224a showed the most potent in vitro activity among the quinolone compounds tested against clinical isolates of gram-positive bacteria. Against gram-negative bacteria, DW-224a was slightly less active than the other fluoroquinolones. The in vivo activities of DW-224a against gram-positive bacteria were more potent than those of other quinolones.

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