Compounds > pleuromutilin
Page last updated: 2024-12-06

pleuromutilin

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

Cross-References

ID SourceID
PubMed CID9886081
CHEMBL ID3989485
SCHEMBL ID16947239
MeSH IDM0045251

Synonyms (38)

Synonym
pleuromuline [inn-french]
glycolic acid 8-ester with octahydro-5,8-dihydroxy-4,6,9,10-tetramethyl-6-vinyl-3a,9-propano-3ah-cyclopentacycloocten-1(4h)-one
nsc 121145
antibiotic bc 757
pleuromulina [inn-spanish]
a 4014c
einecs 204-747-5
acetic acid, hydroxy-, 6-ethenyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3ah-cyclopentacycloocten-8-yl ester, (3as-(3aalpha,4beta,5alpha,6alpha,8beta,9alpha,9abeta,10s*))-
pleuromulinum [inn-latin]
pleuromulin [inn]
14-deoxy-14-((hydroxyacetyl)oxy)mutilin
pleuromulinum
unii-3de4a80mz1
3de4a80mz1 ,
mutilin 14-glycolate
pleuromuline
antibiotic a 40104c
ec 204-747-5
pleuromulina
dtxcid501079582
cas-125-65-5
tox21_113131
dtxsid9048720 ,
acetic acid, hydroxy-, 6-ethenyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3ah-cyclopentacycloocten-8-yl ester, (3as-(3a.alpha.,4.beta.,5.alpha.,6.alpha.,8.beta.,9.alpha.,9a.beta.,10s*))-
bc-757
acetic acid, 2-hydroxy-, (3as,4r,5s,6s,8r,9r,9ar,10r)-6-ethenyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3ah-cyclopentacycloocten-8-yl ester
pleuromutilin [usp impurity]
(3as,4r,5s,6s,8r,9r,9ar,10r)6-ethenyl-5-hydroxy-4,6,9,10-tetramethyl-1-oxodecahydro-3a,9-propano-3ah-cyclopenta[8]annulen-8-yl 2-hydroxyacetate
pleuromutilin [mi]
(+)-pleuromutilin
acetic acid, hydroxy-, (3as,4r,5s,6s,8r,9r,9ar,10r)-6-ethenyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3ah-cyclopentacycloocten-8-yl ester
glycolic acid, 8-ester with octahydro-5,8-dihydroxy-4,6,9,10-tetramethyl-6-vinyl-3a,9-propano-3ah-cyclopentacycloocten-1(4h)-one
valnemulin hydrochloride impurity e [ep impurity]
SCHEMBL16947239
pleuromutilin, >=95%
AKOS032946430
CHEMBL3989485
acetic acid, hydroxy-,(3as,4r,5s,6s,8r,9r,9ar,10r)-6-ethenyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3ah-cyclopentacycloocten-8-ylester

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]

Protein Targets (1)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency29.85540.000811.382244.6684AID686978; AID686979
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (48)

Assay IDTitleYearJournalArticle
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1741704Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 43300 preincubated 16 to 20 hrs followed by subculturing and measured after over night
AID1889916Antibacterial activity against Mycoplasma pneumoniae ATCC29342 assessed as inhibition of bacterial growth incubated for 18 hrs by two-fold serial dilution method2022Bioorganic & medicinal chemistry, 04-01, Volume: 59Design, synthesis and antibacterial evaluation of pleuromutilin derivatives.
AID1855509Inhibition of TGF-beta1/Smad3 signalling in in TGF-beta1 treated mouse NIH3T3 cells transfected with (CAGA)12-Lux reporter gene assessed as suppression ratio at 10 uM incubated for 18 hrs by luciferase based analysis2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of a novel Pleuromutilin derivative as anti-IPF lead compound via high-throughput assay.
AID1833234Antimicrobial activity against Bacillus subtilis assessed as bacterial growth inhibition2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
A Novel Anticancer Stem Cell Compound Derived from Pleuromutilin Induced Necroptosis of Melanoma Cells.
AID1772462Bactericidal activity against Staphylococcus aureus 144 assessed as inhibition of bacterial growth measured after 96 hrs by broth dilution method
AID1741707Bactericidal activity against Staphylococcus aureus 144 preincubated 16 to 20 hrs followed by subculturing and measured after over night
AID1833224Cytotoxicity against human A-375 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
A Novel Anticancer Stem Cell Compound Derived from Pleuromutilin Induced Necroptosis of Melanoma Cells.
AID1638644Antimicrobial activity against Wolbachia wMel infected in Drosophila melanogaster LDW1 cells after 6 days by DAPI-based fluorescence in-situ hybridization assay2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis.
AID1772457Antibacterial activity against Staphylococcus aureus 144 assessed as inhibition of bacterial growth measured after 24 hrs by broth dilution method
AID1833232Antimicrobial activity against Staphylococcus aureus assessed as bacterial growth inhibition2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
A Novel Anticancer Stem Cell Compound Derived from Pleuromutilin Induced Necroptosis of Melanoma Cells.
AID1741702Antibacterial activity against Staphylococcus aureus 144 after 24 hrs by CLSI based broth micro dilution method
AID1833221Cytotoxicity against mouse CT26 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
A Novel Anticancer Stem Cell Compound Derived from Pleuromutilin Induced Necroptosis of Melanoma Cells.
AID1772460Bactericidal activity against Staphylococcus aureus ATCC 29213 assessed as inhibition of bacterial growth measured after 96 hrs by broth dilution method
AID1638643Antimicrobial activity against Wolbachia pipientis infected in Asian tiger mosquito C6/36 cells after 7 days by SYTO11 DNA dye-based confocal imaging analysis2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis.
AID1428686Antibacterial activity against Enterococcus faecium ATCC 35667 after overnight incubation by broth dilution method2017European journal of medicinal chemistry, Feb-15, Volume: 127Design, synthesis and antibacterial evaluation of novel pleuromutilin derivatives possessing piperazine linker.
AID1428683Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after overnight incubation by broth dilution method2017European journal of medicinal chemistry, Feb-15, Volume: 127Design, synthesis and antibacterial evaluation of novel pleuromutilin derivatives possessing piperazine linker.
AID1772459Bactericidal activity against Methycillin-resistant Staphylococcus aureus ATCC 43300 assessed as inhibition of bacterial growth measured after 96 hrs by broth dilution method
AID1772461Bactericidal activity against Staphylococcus aureus AD3 assessed as inhibition of bacterial growth measured after 96 hrs by broth dilution method
AID1741699Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after 24 hrs by CLSI based broth micro dilution method
AID1772454Antibacterial activity against Methycillin-resistant Staphylococcus aureus ATCC 43300 assessed as inhibition of bacterial growth measured after 24 hrs by broth dilution method
AID1833233Antimicrobial activity against Escherichia coli assessed as bacterial growth inhibition2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
A Novel Anticancer Stem Cell Compound Derived from Pleuromutilin Induced Necroptosis of Melanoma Cells.
AID1889917Antibacterial activity against drug resistant Mycoplasma pneumoniae assessed as inhibition of bacterial growth incubated for 18 hrs by two-fold serial dilution method2022Bioorganic & medicinal chemistry, 04-01, Volume: 59Design, synthesis and antibacterial evaluation of pleuromutilin derivatives.
AID1741700Antibacterial activity against Staphylococcus aureus ATCC 29213 after 24 hrs by CLSI based broth micro dilution method
AID1741701Antibacterial activity against Staphylococcus aureus AD3 after 24 hrs by CLSI based broth micro dilution method
AID1889915Antibacterial activity against Mycoplasma pneumoniae ATCC15531 assessed as inhibition of bacterial growth incubated for 18 hrs by two-fold serial dilution method2022Bioorganic & medicinal chemistry, 04-01, Volume: 59Design, synthesis and antibacterial evaluation of pleuromutilin derivatives.
AID1833222Cytotoxicity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
A Novel Anticancer Stem Cell Compound Derived from Pleuromutilin Induced Necroptosis of Melanoma Cells.
AID1889912Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as inhibition of bacterial growth incubated for 18 hrs by two-fold serial dilution method2022Bioorganic & medicinal chemistry, 04-01, Volume: 59Design, synthesis and antibacterial evaluation of pleuromutilin derivatives.
AID1428685Antibacterial activity against Enterococcus faecalis ATCC 29212 after overnight incubation by broth dilution method2017European journal of medicinal chemistry, Feb-15, Volume: 127Design, synthesis and antibacterial evaluation of novel pleuromutilin derivatives possessing piperazine linker.
AID1772458Antibacterial activity against Escherichia coli ATCC 25922 assessed as inhibition of bacterial growth measured after 24 hrs by broth dilution method
AID1772456Antibacterial activity against Staphylococcus aureus AD3 assessed as inhibition of bacterial growth measured after 24 hrs by broth dilution method
AID1833225Cytotoxicity against mouse 4T1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
A Novel Anticancer Stem Cell Compound Derived from Pleuromutilin Induced Necroptosis of Melanoma Cells.
AID1855511Antibacterial activity against Escherichia coli assessed as bacterial growth inhibition incubated for 24 hrs2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of a novel Pleuromutilin derivative as anti-IPF lead compound via high-throughput assay.
AID1889913Antibacterial activity against Enterococcus faecium ATCC19434 assessed as inhibition of bacterial growth incubated for 18 hrs by two-fold serial dilution method2022Bioorganic & medicinal chemistry, 04-01, Volume: 59Design, synthesis and antibacterial evaluation of pleuromutilin derivatives.
AID1428684Antibacterial activity against Staphylococcus aureus ATCC 29213 after overnight incubation by broth dilution method2017European journal of medicinal chemistry, Feb-15, Volume: 127Design, synthesis and antibacterial evaluation of novel pleuromutilin derivatives possessing piperazine linker.
AID1741706Bactericidal activity against Staphylococcus aureus AD3 preincubated 16 to 20 hrs followed by subculturing and measured after over night
AID1855512Antibacterial activity against Bacillus subtilis assessed as bacterial growth inhibition incubated for 24 hrs2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of a novel Pleuromutilin derivative as anti-IPF lead compound via high-throughput assay.
AID1833220Cytotoxicity against human Kasumi 1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
A Novel Anticancer Stem Cell Compound Derived from Pleuromutilin Induced Necroptosis of Melanoma Cells.
AID1772455Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as inhibition of bacterial growth measured after 24 hrs by broth dilution method
AID1889911Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 assessed as inhibition of bacterial growth incubated for 18 hrs by two-fold serial dilution method2022Bioorganic & medicinal chemistry, 04-01, Volume: 59Design, synthesis and antibacterial evaluation of pleuromutilin derivatives.
AID1833223Cytotoxicity against mouse B16-F10 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
A Novel Anticancer Stem Cell Compound Derived from Pleuromutilin Induced Necroptosis of Melanoma Cells.
AID1772463Bactericidal activity against Escherichia coli ATCC 25922 assessed as inhibition of bacterial growth measured after 96 hrs by broth dilution method
AID1741705Bactericidal activity against Staphylococcus aureus ATCC 29213 preincubated 16 to 20 hrs followed by subculturing and measured after over night
AID1889914Antibacterial activity against Staphylococcus epidermidis ATCC12228 assessed as inhibition of bacterial growth incubated for 18 hrs by two-fold serial dilution method2022Bioorganic & medicinal chemistry, 04-01, Volume: 59Design, synthesis and antibacterial evaluation of pleuromutilin derivatives.
AID1855510Antibacterial activity against Staphylococcus aureus assessed as bacterial growth inhibition incubated for 24 hrs2022European journal of medicinal chemistry, Nov-05, Volume: 241Discovery of a novel Pleuromutilin derivative as anti-IPF lead compound via high-throughput assay.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's3 (30.00)24.3611
2020's7 (70.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		2.3110taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
pirfenidone
pirfenidone : A pyridone that is 2-pyridone substituted at positions 1 and 5 by phenyl and methyl groups respectively. An anti-inflammatory drug used for the treatment of idiopathic pulmonary fibrosis.		2.4110pyridoneantipyretic;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
tiamulin
tiamulin: 81723 HFU and tiamutin are for fumarate salt; prevents senescence in ascomycete; pleuromutilin derivative; RN given refers to ((3aS-(3aalpha,4beta,5alpha,6alpha,8beta,9alpha,9abeta,10S*))-isomer. tiamulin : A carbotricyclic compound that is pleuromutilin in which the hydroxyacetate group is replaced by a 2-{[2-(diethylamino)ethyl]sulfanyl}acetate group. An antibacterial drug, tiamulin is used in veterinary medicine (generally as its hydrogen fumarate salt) for the treatment of swine dysentery caused by Serpulina hyodysenteriae.		2.9130carbotricyclic compound;
carboxylic ester;
cyclic ketone;
organic sulfide;
secondary alcohol;
semisynthetic derivative;
tertiary amino compound;
tetracyclic diterpenoid		antibacterial drug
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamide
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide: a TGF-beta type I receptor kinase activity inhibitor		2.4110benzamides;
benzodioxoles;
imidazoles;
pyridines		EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
retapamulin
retapamulin: a synthetic pleuromutilin		2.5820carbotricyclic compound;
carboxylic ester;
cyclic ketone
valnemulin
[no description available]		2.5820
bc-3781
[no description available]		2.2110
minocycline
Minocycline: A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections.. minocycline : A tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5.		2.2110
ConditionIndicatedRelationship StrengthStudiesTrials
Bancroftian Elephantiasis
[description not available]		02.2110
Elephantiasis, Filarial
Parasitic infestation of the human lymphatic system by WUCHERERIA BANCROFTI or BRUGIA MALAYI. It is also called lymphatic filariasis.		02.2110
Onchocerciasis
Infection with nematodes of the genus ONCHOCERCA. Characteristics include the presence of firm subcutaneous nodules filled with adult worms, PRURITUS, and ocular lesions.		07.2110
Malignant Melanoma
[description not available]		02.3110
Melanoma
A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)		07.3110
Cryptogenic Fibrosing Alveolitis
[description not available]		02.4110
Idiopathic Pulmonary Fibrosis
A common interstitial lung disease of unknown etiology, usually occurring between 50-70 years of age. Clinically, it is characterized by an insidious onset of breathlessness with exertion and a nonproductive cough, leading to progressive DYSPNEA. Pathological features show scant interstitial inflammation, patchy collagen fibrosis, prominent fibroblast proliferation foci, and microscopic honeycomb change.		02.4110