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me1036

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

Description

ME1036: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	10300326
CHEMBL ID	387640
SCHEMBL ID	304850
MeSH ID	M0473038

Synonyms (15)

Synonym
CHEMBL387640 ,
me1036
SCHEMBL304850
432038-96-5
33501r83o2 ,
cp-5609
unii-33501r83o2
me-1036
pyridinium, 1-(2-amino-2-oxoethyl)-3-((2-((4s,5r,6s)-2-carboxy-6-((1r)-1-hydroxyethyl)-4-methyl-7-oxo-1-azabicyclo(3.2.0)hept-2-en-3-yl)imidazo(5,1-b)thiazol-7-yl)carbonyl)-, inner salt
bdbm50483328
LZKPUSJSJVEXAW-WDXSGGTDSA-N ,
(1s,5r,6s)-2-[7-(1-carbamoylmethylpyridinium-3-yl)carbonylimidazo[5,1-b]thiazol-2-yl]-6-[(1r)-1-hydroxyethyl]-1-methylcarbapen-2-em-3-carboxylate
Q27256228
(4s,5r,6s)-3-[7-[1-(2-amino-2-oxoethyl)pyridin-1-ium-3-carbonyl]imidazo[5,1-b][1,3]thiazol-2-yl]-6-[(1r)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate
AKOS040751289

Research Excerpts

Effects

Excerpt	Reference	Relevance
"ME1036 has been shown to be strongly active against genotypic penicillin-intermediate S."	( Correlation of the antimicrobial activity of ME1036 with its binding affinities to the penicillin-binding proteins from Streptococcus pneumoniae strains. Hirai, Y; Ida, T; Maebashi, K; Takahata, S; Yamada, K, 2011)	1.35

Dosage Studied

Excerpt	Relevance	Reference
" Compared with vancomycin, ME1036 reduced the bacterial counts in the vegetations at a lower dosage or over a shorter period of administration when it was used for the treatment of MRSA endocarditis."	( Therapeutic effect of ME1036 on endocarditis experimentally induced by methicillin-resistant Staphylococcus aureus. Hirai, Y; Kijima, K; Kurazono, M; Nagura, J; Shitara, E; Sugano, T; Takahata, S; Takayama, Y; Tanaka, Y; Yamada, K; Yonezawa, M, 2005)	0.94

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (10)

Assay ID	Title	Year	Journal	Article
AID284141	Antibacterial activity against Staphylococcus aureus 209P JC1 by agar dilution method	2007	Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1	Synthesis and SAR study of novel 7-(pyridinium-3-yl)-carbonyl imidazo[5,1-b]thiazol-2-yl carbapenems.
AID284147	Antibacterial activity against Moraxella catarrhalis W-0500 by agar dilution method	2007	Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1	Synthesis and SAR study of novel 7-(pyridinium-3-yl)-carbonyl imidazo[5,1-b]thiazol-2-yl carbapenems.
AID519138	Antimicrobial activity against community-acquired methicillin resistant Staphylococcus aureus expressing PVL and mec type IV gene by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	Antimicrobial activities of Ceftaroline and ME1036 tested against clinical strains of community-acquired methicillin-resistant Staphylococcus aureus.
AID284146	Antibacterial activity against Klebsiella pneumoniae GN69 by agar dilution method	2007	Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1	Synthesis and SAR study of novel 7-(pyridinium-3-yl)-carbonyl imidazo[5,1-b]thiazol-2-yl carbapenems.
AID284143	Antibacterial activity against carbapenem and methicillin-resistant Staphylococcus aureus M126HR by agar dilution method	2007	Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1	Synthesis and SAR study of novel 7-(pyridinium-3-yl)-carbonyl imidazo[5,1-b]thiazol-2-yl carbapenems.
AID284144	Antibacterial activity against penicillin-resistant Streptococcus pneumoniae KK133 by agar dilution method	2007	Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1	Synthesis and SAR study of novel 7-(pyridinium-3-yl)-carbonyl imidazo[5,1-b]thiazol-2-yl carbapenems.
AID284145	Antibacterial activity against Escherichia coli NIHJ JC2 by agar dilution method	2007	Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1	Synthesis and SAR study of novel 7-(pyridinium-3-yl)-carbonyl imidazo[5,1-b]thiazol-2-yl carbapenems.
AID284142	Antibacterial activity against methicillin-resistant Staphylococcus aureus M126 by agar dilution method	2007	Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1	Synthesis and SAR study of novel 7-(pyridinium-3-yl)-carbonyl imidazo[5,1-b]thiazol-2-yl carbapenems.
AID284148	Antibacterial activity against beta-lactamase-negative ampicillin-resistant Haemophilus influenzae 870 by agar dilution method	2007	Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1	Synthesis and SAR study of novel 7-(pyridinium-3-yl)-carbonyl imidazo[5,1-b]thiazol-2-yl carbapenems.
AID560209	Binding affinity to methicillin-resistant Staphylococcus aureus MF535HR PBP 2a by competitive binding assay	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	Molecular basis and phenotype of methicillin resistance in Staphylococcus aureus and insights into new beta-lactams that meet the challenge.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	10 (90.91)	29.6817
2010's	1 (9.09)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.95

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

Metric	This Compound (vs All)
Research Demand Index	16.95 (24.57)
Research Supply Index	2.48 (2.92)
Research Growth Index	4.25 (4.65)
Search Engine Demand Index	10.37 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (16.95)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	1 (9.09%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	10 (90.91%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
2-naphthol 2-naphthol: RN given refers to parent cpd. 2-naphthol : A naphthol carrying a hydroxy group at position 2.. naphthols : Any hydroxynaphthalene derivative that has a single hydroxy substituent.	2.03	1	naphthol	antinematodal drug; genotoxin; human urinary metabolite; human xenobiotic metabolite; mouse metabolite; radical scavenger
erythromycin Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively.	2.04	1	cyclic ketone; erythromycin
vancomycin Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.. vancomycin : A complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile.	9.23	5	glycopeptide	antibacterial drug; antimicrobial agent; bacterial metabolite
acetylglucosamine Acetylglucosamine: The N-acetyl derivative of glucosamine.. N-acetyl-beta-D-glucosamine : An N-acetyl-D-glucosamine having beta-configuration at the anomeric centre.	2.04	1	N-acetyl-D-glucosamine	epitope
amoxicillin Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group.	7.04	1	penicillin allergen; penicillin	antibacterial drug
cephalosporin c cephalosporin C: RN given refers to parent cpd; structure in Merck, 9th ed, #1937. cephalosporin C : A cephalosporin antibiotic carrying a 3-acetoxymethyl substituent and a 6-oxo-N(6)-L-lysino group at position 7.	2.73	3	cephalosporin	fungal metabolite
glycidyl nitrate glycidyl nitrate: a nitric oxide donor; structure in first source. peptidoglycan : A peptidoglycosaminoglycan formed by alternating residues of beta-(1->4)-linked N-acetylglucosamine and N-acetylmuramic acid {2-amino-3-O-[(S)-1-carboxyethyl]-2-deoxy-D-glucose} residues. Attached to the carboxy group of the muramic acid is a peptide chain of three to five amino acids.	2.04	1
imipenem, anhydrous Imipenem: Semisynthetic thienamycin that has a wide spectrum of antibacterial activity against gram-negative and gram-positive aerobic and anaerobic bacteria, including many multiresistant strains. It is stable to beta-lactamases. Clinical studies have demonstrated high efficacy in the treatment of infections of various body systems. Its effectiveness is enhanced when it is administered in combination with CILASTATIN, a renal dipeptidase inhibitor.. imipenem : A broad-spectrum, intravenous beta-lactam antibiotic of the carbapenem subgroup.	2.04	1	beta-lactam antibiotic allergen; carbapenems; zwitterion	antibacterial drug
carbapenems [no description available]	3.64	9
beta-lactams 2-azetidinone: structure in first source. azetidin-2-one : An unsubstituted beta-lactam compound.. beta-lactam : A lactam in which the amide bond is contained within a four-membered ring, which includes the amide nitrogen and the carbonyl carbon.	2.04	1	beta-lactam antibiotic allergen; beta-lactam
levofloxacin Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase.	2.04	1	9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid; fluoroquinolone antibiotic; quinolone antibiotic	antibacterial drug; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; topoisomerase IV inhibitor
meropenem Meropenem: A thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.. meropenem : A carbapenemcarboxylic acid in which the azetidine and pyrroline rings carry 1-hydroxymethyl and in which the azetidine and pyrroline rings carry 1-hydroxymethyl and 5-(dimethylcarbamoyl)pyrrolidin-3-ylthio substituents respectively.	2.04	1	alpha,beta-unsaturated monocarboxylic acid; carbapenemcarboxylic acid; organic sulfide; pyrrolidinecarboxamide	antibacterial agent; antibacterial drug; drug allergen
linezolid [no description available]	3.55	2	acetamides; morpholines; organofluorine compound; oxazolidinone	antibacterial drug; protein synthesis inhibitor
clindamycin Clindamycin: An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.. clindamycin : A carbohydrate-containing antibiotic that is the semisynthetic derivative of lincomycin, a natural antibiotic.	2.04	1
n-acetylmuramic acid N-acetylmuramic acid: RN given refers to D-Glucopyranose, (R)-isomer. N-acetyl-D-muramic acid : The pyranose form of N-acetylmuramic acid.	2.04	1	N-acetylmuramic acid
ceftriaxone [no description available]	3.55	2	1,2,4-triazines; 1,3-thiazoles; cephalosporin; oxime O-ether	antibacterial drug; drug allergen; EC 3.5.2.6 (beta-lactamase) inhibitor
ceftazidime [no description available]	3.14	1	cephalosporin; oxime O-ether	antibacterial drug; drug allergen; EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor
way 202196 3-(3-fluoro-4-hydroxyphenyl)-7-hydroxy-1-naphthonitrile: structure in first source	2.03	1
ppi-0903 ceftaroline : A cephalosporin that is the active metabolite of the prodrug ceftaroline fosamil. Used for the treatment of adults with acute bacterial skin and skin structure infections.	3.55	2	1,3-thiazoles; cephalosporin; iminium betaine; organic phosphoramidate; oxime O-ether; thiadiazoles	antibacterial drug; antimicrobial agent; prodrug
sm-216601 SM-216601: exhibits potent activity against methicillin-resistant staphylococci (MRS) and vancomycin-resistant enterococci (VRE); structure in first source	3.14	1
ly-146032 [no description available]	2.04	1	heterodetic cyclic peptide; lipopeptide antibiotic; lipopeptide; macrocycle; macrolide	antibacterial drug; bacterial metabolite; calcium-dependent antibiotics
tetracycline Tetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.. tetracycline : A broad-spectrum polyketide antibiotic produced by the Streptomyces genus of actinobacteria.	2.04	1
ceftobiprole ceftobiprole: BAL5788 is Ceftobiprole medocaril sodium. ceftobiprole : A fifth-generation cephalosporin antibiotic having (E)-[(3'R)-2-oxo[1,3'-bipyrrolidin]-3-ylidene]methyl and [(2Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(hydroxyimino)acetyl]amino side groups located at positions 3 and 7 respectively; developed for the treatment of hospital-acquired pneumonia (HAP, excluding ventilator-associated pneumonia, VAP) and community-acquired pneumonia (CAP).	2.03	1	cephalosporin; thiadiazoles	antimicrobial agent

Condition	Relationship Strength	Studies
Community Acquired Infection [description not available]	2.45	2
Infections, Staphylococcal [description not available]	2.44	2
Staphylococcal Infections Infections with bacteria of the genus STAPHYLOCOCCUS.	2.44	2
Infections, Pneumococcal [description not available]	2.04	1
Pneumococcal Infections Infections with bacteria of the species STREPTOCOCCUS PNEUMONIAE.	2.04	1
Staphylococcal Pneumonia [description not available]	2.04	1
Pneumonia, Staphylococcal Pneumonia caused by infections with bacteria of the genus STAPHYLOCOCCUS, usually with STAPHYLOCOCCUS AUREUS.	2.04	1
Bacterial Pneumonia [description not available]	2.05	1
Bacteremia The presence of viable bacteria circulating in the blood. Fever, chills, tachycardia, and tachypnea are common acute manifestations of bacteremia. The majority of cases are seen in already hospitalized patients, most of whom have underlying diseases or procedures which render their bloodstreams susceptible to invasion.	2.05	1
Pneumonia, Bacterial Inflammation of the lung parenchyma that is caused by bacterial infections.	2.05	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.02	1
Bacterial Endocarditides [description not available]	2.02	1
Endocarditis, Bacterial Inflammation of the ENDOCARDIUM caused by BACTERIA that entered the bloodstream. The strains of bacteria vary with predisposing factors, such as CONGENITAL HEART DEFECTS; HEART VALVE DISEASES; HEART VALVE PROSTHESIS IMPLANTATION; or intravenous drug use.	2.02	1

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