aspoxicillin: structure given in first source
ID Source | ID |
---|---|
PubMed CID | 71961 |
CHEMBL ID | 1318150 |
CHEBI ID | 31240 |
SCHEMBL ID | 34176 |
MeSH ID | M0113423 |
Synonym |
---|
doyle |
ta-058 , |
doyle (tn) |
aspoxicillinum [latin] |
n(sup 4)-methyl-d-asparagininylamoxicillin |
aspoxicilina [spanish] |
ta 058 |
(2s,5r,6r)-6-((2r)-2-((2r)-2-amino-3-(methylcarbamoyl)propionamido)-2-(p-hydroxyphenyl)acetamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid |
ccris 2514 |
aspoxicillan |
aspoxicillin [inn:jan] |
aspoxicilline [french] |
glycinamide, n-methyl-d-asparaginyl-n-(2-carboxy-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)hept-6-yl)-d-2-(4-hydroxyphenyl)-, (2s-(2-alpha,5-alpha,6-beta))- |
NCGC00181352-01 |
aspoxicillin (jan/inn) |
D07469 |
aspoxicillin |
63358-49-6 |
(2s,5r,6r)-6-[[(2r)-2-[[(2r)-2-amino-4-(methylamino)-4-oxobutanoyl]amino]-2-(4-hydroxyphenyl)acetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid |
dtxcid4026921 |
dtxsid6046921 , |
tox21_112810 |
cas-63358-49-6 |
CHEMBL1318150 |
chebi:31240 , |
aspoxicilline |
aspoxicillinum |
aspoxicilina |
unii-0745kno26j |
0745kno26j , |
aspoxicillin [mi] |
aspoxicillin [who-dd] |
aspoxicillin [mart.] |
aspoxicillin [inn] |
SCHEMBL34176 |
(2s,5r,6r)-6-[[(2r)-2-[[(2r)-2-amino-4-(methylamino)-4-oxo-butanoyl]amino]-2-(4-hydroxyphenyl)acetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid |
glycinamide, n-methyl-d-asparaginyl-n-(2-carboxy-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-6-yl)-d-2-(4-hydroxyphenyl)-, [2s-(2?,5?,6?)]-; aspc; aspoxicillin; doyle; ta 058 |
(2s,5r,6r)-6-[[(2r)-2-[[(2r)-2-amino-4-methylamino-4-oxobutanoyl]amino]-2-(4-hydroxyphenyl)acetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid |
HY-135842 |
DB13816 |
BHELIUBJHYAEDK-OAIUPTLZSA-N |
Q27114235 |
CS-0114376 |
MS-29166 |
gtpl12293 |
AKOS040732482 |
Aspoxicillin shows a slightly longer half-life elimination than semi-synthetic penicillins.
Excerpt | Reference | Relevance |
---|---|---|
" In contrast to available semi-synthetic penicillins, aspoxicillin shows a slightly longer half-life elimination." | ( Pharmacokinetics of aspoxicillin in subjects with normal and impaired renal function. Geyer, J; Höffler, D; Koeppe, P, 1988) | 0.85 |
"The serum concentrations, urinary and biliary excretions of six penicillin derivatives including aspoxicillin (ASPC) were studied in rats and the correlation between the values of pharmacokinetic parameters thus obtained and the Rm values measured by means of reversed phase TLC were analyzed." | ( Effect of the hydroxyl group of the p-hydroxyphenyl moiety of aspoxicillin, a semisynthetic penicillin, on its pharmacokinetic property. Maezawa, I; Matsushita, T; Okuno, S; Sakuma, Y; Yamaguchi, T, 1988) | 0.73 |
Excerpt | Reference | Relevance |
---|---|---|
"We studied clinical effects of ceftazidime (CAZ) alone or in combination with aspoxicillin (ASPC) against various infections in obstetric and gynecological patients." | ( [A clinical study on the efficacy of ceftazidime alone or in combination with aspoxicillin against infections in obstetric and gynecological patients]. Chimura, T; Funayama, T; Hirayama, T; Kanasugi, H; Miyata, R; Morisaki, N; Nara, N; Oda, T; Saito, N; Sato, S, 1993) | 0.74 |
Excerpt | Reference | Relevance |
---|---|---|
"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 |
Excerpt | Relevance | Reference |
---|---|---|
" Dosage reduction factors are then derived which allow appropriate dosages to be established for the substances under examination." | ( Pharmacokinetics of aspoxicillin in subjects with normal and impaired renal function. Geyer, J; Höffler, D; Koeppe, P, 1988) | 0.6 |
" ASPC was administered in 3 or 4 divided doses at a daily dosage ranging from 21 to 98 mg/kg by 30 minutes drip infusion or intravenous injection to 29 patients (16 cases of pneumonia, 8 cases of tonsillitis, 3 cases of bronchitis, 1 case of urinary tract infection, 1 case of impetigo) and the following clinical results were obtained: excellent; 11 cases, good; 11 cases, fair; 3 cases, poor; 1 case." | ( [Clinical evaluation of aspoxicillin in children]. Ito, S; Mikawa, H; Mochizuki, Y; Ohkubo, H, 1985) | 0.58 |
" ASPC was intravenously administered in 3 or 4 divided doses at a daily dosage ranging from 83." | ( [Clinical studies of aspoxicillin in pediatrics]. Haruta, T; Kobayashi, Y; Kuroki, S; Okura, K, 1985) | 0.59 |
" ASPC was injected by drip infusion and the dosage was 63-117 mg/kg/day in 3 and 4 times a day." | ( [The therapeutic effects of aspoxicillin on various infectious diseases in children]. Araki, K; Kitamura, I; Maeda, A; Ogura, H; Ohara, Y; Shiraishi, T; Tone, Y; Wakiguchi, H, 1985) | 0.56 |
" A dose response was seen among the 3 dosage levels." | ( [Fundamental and clinical studies of aspoxicillin in the pediatric field]. Fujimoto, T; Kawakami, A; Koga, T; Motohiro, T; Nishiyama, T; Sakata, Y; Shimada, Y; Tanaka, K; Tominaga, K; Tomita, N, 1985) | 0.54 |
" Most of urinary recovery was excreted within 4 hours after administration regardless of dose levels, frequency of dosing or administration route." | ( [Safety and pharmacology of aspoxicillin in healthy volunteers]. Maezawa, I; Matsumoto, K; Nagatake, T; Sakuma, Y; Shishido, H; Uzuka, Y; Yamaguchi, T; Yamamoto, M, 1985) | 0.56 |
Class | Description |
---|---|
peptide | Amide derived from two or more amino carboxylic acid molecules (the same or different) by formation of a covalent bond from the carbonyl carbon of one to the nitrogen atom of another with formal loss of water. The term is usually applied to structures formed from alpha-amino acids, but it includes those derived from any amino carboxylic acid. X = OH, OR, NH2, NHR, etc. |
[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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
phosphopantetheinyl transferase | Bacillus subtilis | Potency | 15.8489 | 0.1413 | 37.9142 | 100.0000 | AID1490 |
peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 36.1254 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 34 (60.71) | 18.7374 |
1990's | 18 (32.14) | 18.2507 |
2000's | 1 (1.79) | 29.6817 |
2010's | 2 (3.57) | 24.3611 |
2020's | 1 (1.79) | 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 moderate demand-to-supply ratio for research on this compound.
| This Compound (19.89) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 6 (10.53%) | 5.53% |
Reviews | 3 (5.26%) | 6.00% |
Case Studies | 7 (12.28%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 41 (71.93%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |