cefquinome: broad spectrum antibiotic; RN given refers to (6R(6alpha,7beta(Z)-isomer); structure given in first source
ID Source | ID |
---|---|
PubMed CID | 5464355 |
CHEMBL ID | 1631107 |
SCHEMBL ID | 149896 |
MeSH ID | M0186653 |
Synonym |
---|
cobactan [veterinary] (tn) |
cefquinome (inn) |
D07652 |
84957-30-2 |
cefquinome |
(6r,7r)-7-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-8-oxo-3-(5,6,7,8-tetrahydroquinolin-1-ium-1-ylmethyl)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate |
1-[[(6r,7r)-7-[[(2z)-(2-amino-4-thiazolyl)(methoxyimino)acetyl]amino]-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]-5,6,7,8-tetrahydro-quinolinium inner salt |
hr111v |
cobactan |
CHEMBL1631107 |
cefquinomum |
cefquinoma |
unii-z74s078cwp |
cefquinome [inn:ban] |
z74s078cwp , |
cefquinomum [inn-latin] |
1-(((6r,7r)-7-(2-(2-amino-4-thiazolyl)glyoxylamido)-2-carboxy-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-en-3-yl)methyl)-5,6,7,8-tetrahydroquinolinium hydroxide, inner salt, 7(sup 2)-(z)-(o-methyloxime) |
cefquinoma [inn-spanish] |
quinolinium, 1-((7-(((2-amino-4-thiazolyl)(methoxyimino)acetyl)amino)-2-carboxy-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-en-3-yl)methyl)-5,6,7,8-tetrahydro-, hydroxide, inner salt, (6r-(6.alpha.,7.beta.(z)))- |
1-(((6r,7r)-7-(2-(2-amino-4-thiazolyl)glyoxylamido)-2-carboxy-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-en-3-yl)methyl)-5,6,7,8-tetrahydroquinolinium hydroxide, inner salt, 72-(z)-(o-methyloxime) |
cefquinome [inn] |
cefquinome [mi] |
SCHEMBL149896 |
AKOS025402360 |
DTXSID00894103 |
Cefquinome (CEQ) is a novel β-lactam antibiotic that exhibits excellent antibacterial activity against Staphylococcus aureus. Cephalosporin (CFQ) has been widely used for treating porcine or bovine respiratory infection, Bovine mastitis and other diseases.
Excerpt | Reference | Relevance |
---|---|---|
"Cefquinome has a broad spectrum of antibacterial activity and was developed especially for use in animals. " | ( Development and validation of a high-performance liquid chromatography method for determination of cefquinome concentrations in sheep plasma and its application to pharmacokinetic studies. Altan, F; Elmas, M; Uney, K, 2011) | 2.03 |
"Cefquinome has a broad spectrum of antibacterial activity and was developed especially for use in animals. " | ( Development and validation of a high-performance liquid chromatography method for determination of cefquinome concentrations in sheep plasma and its application to pharmacokinetic studies. Altan, F; Elmas, M; Uney, K, 2011) | 2.03 |
This work aims to study the pharmacokinetic (PK) and pharmacodynamic (PD) modeling following intramammary administration of cefquinome against S. After IV injection, mean distribution half-life was longer in goslings.
Excerpt | Reference | Relevance |
---|---|---|
"The purpose of the present clinical studies was to determine the clinical efficacy of a combined parenteral and oral treatment with Bisolvon in combination with antibiotics in bovines suffering from acute respiratory disease." | ( [Treatment of acute respiratory tract diseases in cattle with Bisolvon in combination with either enrofloxacin, cefquinome, ceftiofur or florfenicol]. Hamel, U; Philipp, H; Quirke, JF; Schmidt, H, 1998) | 0.51 |
"The aim of this study was to develop a rapid and sensitive method for the quantification of cefquinome in animal plasma and bronchoalveolar lavage (BAL) fluid using high-performance liquid chromatography combined with electrospray tandem mass spectrometry (LC-ESI-MS/MS)." | ( Determination of cefquinome in pig plasma and bronchoalveolar lavage fluid by high-performance liquid chromatography combined with electrospray ionization mass spectrometry. Croubels, S; De Backer, P; Maes, A; Maes, D; Meyns, T; Sustronck, B, 2007) | 0.9 |
A study on bioavailability and pharmacokinetics of cefquinome in piglets was conducted after intravenous (i.i. IV, IM, or PO) injection. After IM administration of injectable cefquinome sulfate, bioavailability of the drug was higher in goslings (113.5 mg/kg)
Pharmacokinetic characteristics were evaluated following intramuscular administration of CEF-GMS or Cefquinome sulfate injection (CEF-Inj) in pigs at a dosage of 4 mg CEF/kg body weight. In conjunction with the data on MIC, MBC values and the ex vivo bactericidal activity in serum, the present results allowed prediction that a single cefquinomes dosage of 2 mg/kg may be effective in dogs against K. Escherichia coli.
Excerpt | Relevance | Reference |
---|---|---|
" Drug resistance was determined by using break-points, which consider the dosage regimen and pharmacokinetics of the veterinary antimicrobials investigated." | ( In vitro efficacy of cefquinome (INN) and other anti-infective drugs against bovine bacterial isolates from Belgium, France, Germany, The Netherlands, and the United Kingdom. Böttner, A; Humke, R; Schmid, P, 1995) | 0.61 |
" Based on AUC values, total cefquinome concentrations in PELF were one-third of total plasma concentrations after intravenous administration together with shorter time above Minimum Inhibitory Concentrations (T > MIC) in PELF, thus twice daily dosing may be required when treating lower airway infections in horses." | ( Antimicrobial disposition in pulmonary epithelial lining fluid of horses, part III. cefquinome. Baptiste, KE; Friis, C; Winther, L, 2011) | 0.89 |
"To compare the pharmacokinetics of the fourth generation cephalosporin, cefquinome, in neonatal foals, 6-week-old foals and mature New Forest ponies in order to recommend appropriate dosage regimens for use of this drug." | ( Comparing the pharmacokinetics of a fourth generation cephalosporin in three different age groups of New Forest ponies. Fink-Gremmels, J; Haritova, A; Heil, BA; Smiet, E; Wijnberg, ID, 2012) | 0.61 |
"Commonly used dosing regimens should be critically evaluated in neonatal foals due to the higher volume of distribution of less lipophilic drugs in this age group." | ( Comparing the pharmacokinetics of a fourth generation cephalosporin in three different age groups of New Forest ponies. Fink-Gremmels, J; Haritova, A; Heil, BA; Smiet, E; Wijnberg, ID, 2012) | 0.38 |
" These data may be used as a rational basis for setting dosing schedules, which optimize clinical efficacy and minimize the opportunities for emergence of resistant organisms." | ( Pharmacokinetic/pharmacodynamic relationship of cefquinome against Pasteurella multocida in a tissue-cage model in yellow cattle. Ding, H; He, L; Shan, Q; Wang, J; Yang, F; Zeng, Z, 2014) | 0.66 |
"In order to provide some basis for effective dosage regimens that optimize efficacy with respect to bacteriological and clinical cures, the in vivo activity of cefquinome against a clinical Escherichia coli (E." | ( Response of a clinical Escherichia coli strain to repeated cefquinome exposure in a piglet tissue-cage model. Ding, H; Gu, M; Gu, X; Shen, X; Xiong, M; Yang, Y; Zhang, L; Zhang, N, 2015) | 0.86 |
" The percentage of a 24-h dosing interval that the unbound serum cefquinome concentrations exceeded the MIC (fT > MIC) were the pharmacokinetic (PK)-pharmacodynamic (PD) parameter that best correlated with efficacy (R(2) 86." | ( In vivo activity of cefquinome against Riemerella anatipestifer using the pericarditis model in the duck. Cao, C; Lu, Y; Qiu, Z; Qu, Y; Sun, M; Zeng, Z; Zhang, Y; Zhong, J, 2016) | 1 |
" The PK/PD studies demonstrated that the percentage of time that serum drug levels were above the MIC of free drug (%ƒT>MIC) in a 24-h dosing interval was the primary index driving the efficacy of both inoculum sizes (R(2) = 91% and R(2) = 63%)." | ( In Vivo Pharmacodynamics of Cefquinome in a Neutropenic Mouse Thigh Model of Streptococcus suis Serotype 2 at Varied Initial Inoculum Sizes. Guo, C; Liao, X; Liu, Y; Sun, J; Wang, F; Wang, M; Xiao, X; Yan, C, 2016) | 0.73 |
" Pharmacokinetic characteristics were evaluated following intramuscular administration of CEF-GMS or Cefquinome sulfate injection (CEF-Inj) in pigs at a dosage of 4 mg CEF/kg body weight." | ( Preparation and evaluation of cefquinome-loaded gelatin microspheres and the pharmacokinetics in pigs. Cao, J; Dai, W; He, B; Lei, Z; Lu, Z; Yang, B; Zhang, S; Zhou, H, 2018) | 0.99 |
" In this study, a physiologically based pharmacokinetic (PBPK) model was calibrated based on the published data and a microdialysis experiment to assess the dosage efficiency and food safety." | ( A physiologically based pharmacokinetic model to optimize the dosage regimen and withdrawal time of cefquinome in pigs. Cai, X; Hou, Y; Huang, L; Liu, Z; Ma, W; Mi, K; Pan, Y; Sun, L; Xu, X; Zhou, K, 2023) | 1.13 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
GLS protein | Homo sapiens (human) | Potency | 6.3096 | 0.3548 | 7.9355 | 39.8107 | AID624170 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID70951 | Antibacterial activity against Escherichia coli TEM | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins. |
AID542766 | Antimicrobial activity against Escherichia coli PA11 expressing aac(6')-Ib-cr, qnrS1 and qepA genes by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | High prevalence of plasmid-mediated quinolone resistance determinants qnr, aac(6')-Ib-cr, and qepA among ceftiofur-resistant Enterobacteriaceae isolates from companion and food-producing animals. |
AID209892 | Antibacterial activity against Streptococcus pneumoniae | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins. |
AID542770 | Antimicrobial activity against Escherichia coli J53 transformed with pHND2 carrying qnrB6 and CTX-M-9G genes by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | High prevalence of plasmid-mediated quinolone resistance determinants qnr, aac(6')-Ib-cr, and qepA among ceftiofur-resistant Enterobacteriaceae isolates from companion and food-producing animals. |
AID542769 | Antimicrobial activity against Escherichia coli J53 transformed with pHND1 carrying DHA-1 gene by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | High prevalence of plasmid-mediated quinolone resistance determinants qnr, aac(6')-Ib-cr, and qepA among ceftiofur-resistant Enterobacteriaceae isolates from companion and food-producing animals. |
AID542768 | Antimicrobial activity against Escherichia coli J53 by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | High prevalence of plasmid-mediated quinolone resistance determinants qnr, aac(6')-Ib-cr, and qepA among ceftiofur-resistant Enterobacteriaceae isolates from companion and food-producing animals. |
AID68060 | Antibacterial activity against Enterococcus faecium | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins. |
AID542773 | Antimicrobial activity against Escherichia coli J53 transformed with pHNPA1 carrying qnrB6 gene by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | High prevalence of plasmid-mediated quinolone resistance determinants qnr, aac(6')-Ib-cr, and qepA among ceftiofur-resistant Enterobacteriaceae isolates from companion and food-producing animals. |
AID68010 | Antibacterial activity against Enterobacter cloacae 265A | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins. |
AID542737 | Antimicrobial activity against Klebsiella pneumoniae D24 expressing aac(6')-Ib-cr and CTX-M-9G genes by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | High prevalence of plasmid-mediated quinolone resistance determinants qnr, aac(6')-Ib-cr, and qepA among ceftiofur-resistant Enterobacteriaceae isolates from companion and food-producing animals. |
AID542742 | Antimicrobial activity against Citrobacter freundii D26 expressing qnrB6 and CTX-M-9G genes by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | High prevalence of plasmid-mediated quinolone resistance determinants qnr, aac(6')-Ib-cr, and qepA among ceftiofur-resistant Enterobacteriaceae isolates from companion and food-producing animals. |
AID210248 | Antibacterial activity against Streptococcus pyogenes | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins. |
AID542759 | Antimicrobial activity against Escherichia coli Du19 expressing qnrB6 and CTX-M-9G genes by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | High prevalence of plasmid-mediated quinolone resistance determinants qnr, aac(6')-Ib-cr, and qepA among ceftiofur-resistant Enterobacteriaceae isolates from companion and food-producing animals. |
AID68012 | Antibacterial activity against Enterobacter cloacae EB5 | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins. |
AID95918 | Antibacterial activity against Klebsiella pneumoniae X26 | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins. |
AID542735 | Antimicrobial activity against Klebsiella pneumoniae D10 expressing aac(6')-Ib-cr, qnrB4, CTX-M-1G and DHA-1 genes by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | High prevalence of plasmid-mediated quinolone resistance determinants qnr, aac(6')-Ib-cr, and qepA among ceftiofur-resistant Enterobacteriaceae isolates from companion and food-producing animals. |
AID542772 | Antimicrobial activity against Escherichia coli J53 transformed with pHNDU1 carrying qnrB6 gene by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | High prevalence of plasmid-mediated quinolone resistance determinants qnr, aac(6')-Ib-cr, and qepA among ceftiofur-resistant Enterobacteriaceae isolates from companion and food-producing animals. |
AID542771 | Antimicrobial activity against Escherichia coli J53 transformed with pHND3 carrying qnrB6 gene by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | High prevalence of plasmid-mediated quinolone resistance determinants qnr, aac(6')-Ib-cr, and qepA among ceftiofur-resistant Enterobacteriaceae isolates from companion and food-producing animals. |
AID164241 | Antibacterial activity against Pseudomonas aeruginosa PS18 | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins. |
AID205379 | Antibacterial activity against Serratia marcescens SE3 | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins. |
AID69605 | Antibacterial activity against Escherichia coli EC14 | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins. |
AID164246 | Antibacterial activity against Pseudomonas aeruginosa X528 | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins. |
AID206865 | Antibacterial activity against penicillin G resistance Staphylococcus aureus | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins. |
AID95913 | Antibacterial activity against Klebsiella pneumoniae 1082E | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins. |
AID206866 | Antibacterial activity against penicillin G susceptible Staphylococcus aureus | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 10 (10.00) | 18.2507 |
2000's | 12 (12.00) | 29.6817 |
2010's | 63 (63.00) | 24.3611 |
2020's | 15 (15.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.
| This Compound (48.55) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 21 (20.19%) | 5.53% |
Reviews | 2 (1.92%) | 6.00% |
Case Studies | 1 (0.96%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 80 (76.92%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |