Page last updated: 2024-12-06

cefaloram

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Cefaloram is a broad-spectrum cephalosporin antibiotic. It is active against a wide range of gram-positive and gram-negative bacteria, including Staphylococcus aureus, Streptococcus pneumoniae, Escherichia coli, and Klebsiella pneumoniae. Cefaloram is typically administered intravenously or intramuscularly. It is used to treat a variety of bacterial infections, including pneumonia, urinary tract infections, and skin infections. Cefaloram is a synthetic antibiotic, and its synthesis involves multiple steps. It is studied because it is a promising therapeutic agent for the treatment of bacterial infections. It is also studied because it has a unique pharmacological profile, which may make it a good candidate for future drug development.'

cefaloram: RN given refers to parent cpd; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

cefaloram : A cephalosporin derivative with potent antibacterial activity which binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division, inactivation of which interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity, resulting in the weakening of the bacterial cell wall and causing cell lysis. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID68940
CHEMBL ID1700858
CHEBI ID192380
SCHEMBL ID612836
MeSH IDM0166681

Synonyms (29)

Synonym
smr001554387
MLS002666834
(6r,7r)-3-(acetoxymethyl)-8-oxo-7-(2-phenylacetamido)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
NCGC00160359-01
cefaloram
(6r,7r)-3-(acetyloxymethyl)-8-oxo-7-[(2-phenylacetyl)amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
859-07-4
(6r,7r)-3-[(acetyloxy)methyl]-8-oxo-7-(2-phenylacetamido)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
3-(acetoxymethyl)-8-oxo-7-(phenylacetamido)-5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid
cefaloramo
cephaloram
CHEBI:192380
cefaloramum
dtxsid9046106 ,
dtxcid7026106
tox21_111761
cas-859-07-4
CHEMBL1700858
cefaloramum [inn-latin]
(6r,7r)-3-(acetoxymethyl)-8-oxo-7-(2-phenylacetamido)-5-thia-1-azabicyclo(4.2.0)oct-2-en-2-carbonsaeure
einecs 212-725-1
unii-k3086gqj9z
cefaloramo [inn-spanish]
k3086gqj9z ,
cefaloram [inn:ban]
cefaloram [inn]
SCHEMBL612836
Q27281875
(6r,7r)-3-(acetoxymethyl)-8-oxo-7-(2-phenylacetamido)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylicacid

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
antibacterial drugA drug used to treat or prevent bacterial infections.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
cephalosporinA class of beta-lactam antibiotics differing from the penicillins in having a 6-membered, rather than a 5-membered, side ring. Although cephalosporins are among the most commonly used antibiotics in the treatment of routine infections, and their use is increasing over time, they can cause a range of hypersensitivity reactions, from mild, delayed-onset cutaneous reactions to life-threatening anaphylaxis in patients with immunoglobulin E (IgE)-mediated allergy.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency79.43280.631035.7641100.0000AID504339
thioredoxin reductaseRattus norvegicus (Norway rat)Potency12.58930.100020.879379.4328AID588453
TDP1 proteinHomo sapiens (human)Potency25.92900.000811.382244.6684AID686979
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency7.07950.707912.194339.8107AID720542
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency112.20203.548119.542744.6684AID743266
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency12.58930.425612.059128.1838AID504891
DNA polymerase eta isoform 1Homo sapiens (human)Potency25.11890.100028.9256213.3130AID588591
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency2.51190.050127.073689.1251AID588590
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (38)

Assay IDTitleYearJournalArticle
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1117380Antimicrobial activity against methicillin-resistant Staphylococcus aureus 134/93 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1812374Stability of the compound assessed as Klebsiella pneumoniae beta-lactamase IMP-28-mediated degradation by measuring appearance of vinyl protons release measured after 120 mins by NMR spectra2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Novel Cephalosporin Conjugates Display Potent and Selective Inhibition of Imipenemase-Type Metallo-β-Lactamases.
AID1117390Antimicrobial activity against Pseudomonas aeruginosa K799/61 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1538444Prodrug activation in Escherichia coli CFT073 harboring CTX-M-1 assessed as bacterial CTX-M-1-mediated compound hydrolysis incubated for 1 hr by 1H-NMR analysis2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Exploitation of Antibiotic Resistance as a Novel Drug Target: Development of a β-Lactamase-Activated Antibacterial Prodrug.
AID1117382Antimicrobial activity against vancomycin-resistant Enterococcus faecalis 1528 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1538463Selectivity ratio of MIC for ciprofloxacin-susceptible Escherichia coli CFT073 harboring pSU18 to MIC for ciprofloxacin-susceptible Escherichia coli DH5[alpha]2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Exploitation of Antibiotic Resistance as a Novel Drug Target: Development of a β-Lactamase-Activated Antibacterial Prodrug.
AID1117369Antimicrobial activity against Bacillus subtilis ATCC 6633 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1117385Antimicrobial activity against Micrococcus luteus ATCC 10240 assessed as unclear inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1117370Antimicrobial activity against Bacillus subtilis ATCC 6633 assessed as partially clear inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1117374Antimicrobial activity against Staphylococcus aureus Efs1 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1117377Antimicrobial activity against Staphylococcus aureus Efs4 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1117372Antimicrobial activity against Staphylococcus aureus SG511 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1538434Growth inhibition of ciprofloxacin-susceptible Escherichia coli DH5[alpha] incubated for 18 hrs by broth microdilution method2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Exploitation of Antibiotic Resistance as a Novel Drug Target: Development of a β-Lactamase-Activated Antibacterial Prodrug.
AID1117384Antimicrobial activity against Micrococcus luteus ATCC 10240 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1538443Growth inhibition of Escherichia coli CFT073 harboring pSU18 and CTX-M-15 incubated for 18 hrs by broth microdilution method2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Exploitation of Antibiotic Resistance as a Novel Drug Target: Development of a β-Lactamase-Activated Antibacterial Prodrug.
AID1538435Growth inhibition of Escherichia coli DH5[alpha] expressing ESBL TEM-116 incubated for 18 hrs by broth microdilution method2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Exploitation of Antibiotic Resistance as a Novel Drug Target: Development of a β-Lactamase-Activated Antibacterial Prodrug.
AID1538442Growth inhibition of ciprofloxacin-susceptible Escherichia coli CFT073 harboring pSU18 incubated for 18 hrs by broth microdilution method2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Exploitation of Antibiotic Resistance as a Novel Drug Target: Development of a β-Lactamase-Activated Antibacterial Prodrug.
AID1117398Antimicrobial activity against Pseudomonas aeruginosa K799/WT assessed as faint inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1117393Antimicrobial activity against Escherichia coli SG458 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1538436Substrate activity at recombinant Escherichia coli full-length N-terminal His-tagged AmpC (20 to 377 residues) expressed in Escherichia coli assessed as Kcat to Km ratio measured every 20 secs for 1 hr by UV absorbance2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Exploitation of Antibiotic Resistance as a Novel Drug Target: Development of a β-Lactamase-Activated Antibacterial Prodrug.
AID1117396Antimicrobial activity against Mycobacterium vaccae IMET assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902 (14.29)18.7374
1990's0 (0.00)18.2507
2000's3 (21.43)29.6817
2010's5 (35.71)24.3611
2020's4 (28.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.55

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.55 (24.57)
Research Supply Index2.77 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.55)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (7.14%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (92.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]