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 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
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. [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]
| ID Source | ID |
|---|---|
| PubMed CID | 656958 |
| CHEMBL ID | 1234521 |
| CHEBI ID | 44137 |
| SCHEMBL ID | 18232392 |
| MeSH ID | M0062587 |
| Synonym |
|---|
| so 14055 |
| sq-14055 |
| CHEMBL1234521 |
| chebi:44137 , |
| MUL , |
| tiamulin pamoate |
| ((2-(diethylamino)ethyl)thio)acetic acid 8-ester with (3as,4r,5s,6s,8r,9r,9ar,10r)-octahydro-5,8-dihydroxy-4,6,9,10-tetramethyl-6-vinyl-3a,9-propano-3ah-cyclopentacycloocten-1(4h)-one |
| 14-deoxy-14-((2-diethylaminoethyl-thio)-acetoxy)mutiline |
| tiamulinum [inn-latin] |
| 2-(diethylaminoethyl)thioacetoxymutilin |
| acetic acid, ((2-(diethylamino)ethyl)thio)-, 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*))- |
| brn 2229396 |
| sq 14055 |
| denagard |
| einecs 259-580-0 |
| tiamuline [inn-french] |
| hsdb 7026 |
| tiavet p |
| ((2-(diethylamino)ethyl)thio)acetic acid 8-ester with (3as,4r,5s,6s,8r,9r,9ar,10r)-octahydro-5,8-dihydroxy-4,6,9,10)-tetramethyl-6-vinyl-3a,9-propano-3ah-cyclopentacycloocten-1(4h)-one |
| tiamulina [inn-spanish] |
| tiamulina [italian] |
| thiamutilin |
| tiamutin |
| tiamulin (usp/inn) |
| denagard (tn) |
| D06127 |
| tiamulin |
| 55297-95-5 |
| AC1LCVRY , |
| dtxcid00819917 |
| tox21_112539 |
| cas-55297-95-5 |
| dtxsid2046701 , |
| (3as,4r,5s,6s,8r,9r,9ar,10r)-6-ethenyl-5-hydroxy-4,6,9,10-tetramethyl-1-oxodecahydro-3a,9-propanocyclopenta[8]annulen-8-yl {[2-(diethylamino)ethyl]sulfanyl}acetate |
| AKOS016010156 |
| ((2-(diethylamino)ethyl)thio)-, 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*))- |
| unii-e38wz4u54r |
| tiamulina |
| tiamulinum |
| e38wz4u54r , |
| acetic acid, ((2-(diethylamino)ethyl)thio)-, (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 |
| tiamulin [usan:usp:inn:ban] |
| tiamuline |
| [[2-(diethylamino)ethyl]thio]acetic acid 8-ester with (3as,4r,5s,6s,8r,9r,9ar,10r)-octahydro-5,8-dihydroxy-4,6,9,10)-tetramethyl-6-vinyl-3a,9-propano-3ah-cyclopentacycloocten-1(4h)-one |
| tiamulin [hsdb] |
| tiamulin [usp-rs] |
| tiamulin [usp monograph] |
| tiamulin [mi] |
| tiamulin [usan] |
| ((2-(diethylamino)ethyl)thio)-, 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*))- |
| tiamulin [mart.] |
| tiamulin [green book] |
| tiamulin [inn] |
| SCHEMBL18232392 |
| (3as,4r,5s,6s,8r,9r,9ar,10r)-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-6-vinyldecahydro-3a,9-propanocyclopenta[8]annulen-8-yl {[2-(diethylamino)ethyl]sulfanyl}acetate |
| 3-[2-[3-[[4-[[[(2r,3s,4r,5r)-5-(6-aminopurin-9-yl)-4-hydroxy-3-phosphonooxy-tetrahydrofuran-2-yl]methoxy-hydroxy-phosphoryl]oxy-hydroxy-phosphoryl]oxy-2-hydroxy-3,3-dimethyl-butanoyl]amino]propanoylamino]ethylsulfanylcarbonyl]-4-hydroxy-4-(2-naphthyl)buta |
| tiamulin; (3as,4r,5s,6s,8r,9r,9ar,10r)-6-ethenyl-5-hydroxy- 4,6,9,10-tetramethyl-1-oxodecahydro-3a,9-propano-3ah-cyclopentacycloocten-8-yl [[2-(diethylamino)ethyl]sulfanyl]acetate |
| HY-B2060 |
| DB11468 |
| Q7800111 |
| STL559052 |
| BBL036673 |
| CS-0014153 |
| acetic acid, [[2-(diethylamino)ethyl]thio]-,(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 |
| bdbm50569645 |
| tiamulin (usan:usp:inn:ban) |
| ((2-(diethylamino)ethyl)thio)-, 6-ethenyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3ah-cyclopentacycloocten-8-yl ester (3as-(3a-alpha,4beta,5alpha,6alpha,8beta,9alpha,9a-beta,10s*))- |
| tiamulin (usp monograph) |
| tiamulina (inn-spanish) |
| tiamulinum (latin) |
| tiamulin (usp-rs) |
| tiamulinum (inn-latin) |
| (3as,4r,5s,6s,8r,9r,9ar,10r)-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-6-vinyldecahydro-3a,9-propanocyclopenta(8)annulen-8-yl ((2-(diethylamino)ethyl)sulfanyl)acetate |
| tiamuline (inn-french) |
| tiamulin (mart.) |
| denagard soluble antibiotic |
Tiamulin (TML) is a pleuromutilin antibiotic and mainly used to treat pulmonary and gastrointestinal infections. Tiamulin is an antimicrobial widely used in veterinary practice to treat dysentery and pneumonia in pigs and poultry.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Tiamulin resistance has not been reported in The Netherlands before." | ( [Multiresistant Brachyspira hyodysenteriae in a Dutch sow herd]. de Winne, RT; Dierikx, CM; Duinhof, TF; Koene, MG; Mevius, DJ; van Beers-Schreurs, HM; van Bergen, MA; Veldman, KT, ) | 0.85 |
An investigation involving 640 turkeys demonstrated that the inclusion of lasalocid continuously from day-old to 16 weeks of age, at levels up to 375 ppm in the feed, produced no adverse effects.
| Excerpt | Reference | Relevance |
|---|---|---|
| "An investigation involving 640 turkeys demonstrated that the inclusion of lasalocid continuously from day-old to 16 weeks of age, at levels up to 375 ppm in the feed, produced no adverse effects; furthermore, the inclusion of 125 ppm lasalocid in the feed was compatible with the administration of 250 ppm tiamulin in the drinking water continuously for five days to turkeys over the same age range." | ( Safety of lasalocid in turkeys and its compatibility with tiamulin. Comben, N; Fairley, C; Lodge, NJ; Roberts, NL, 1988) | 0.69 |
| " In addition the efficacy of a safe dose for prophylactic treatment of dysentery was controlled." | ( [Toxicity of the combination of salinomycin and tiamulin in swine]. Bollwahn, W; Büsing, S; Wendt, M, 1997) | 0.55 |
| "The characteristics of the toxic interaction between monensin and tiamulin were investigated in rats." | ( Studies on the toxic interaction between monensin and tiamulin in rats: toxicity and pathology. Bajnógel, J; Laczay, P; Móra, Z; Szücs, G; Varga, A, 2000) | 0.79 |
| " The toxic action of the drug may be connected with the extent and routes of its biotransformation." | ( Cytotoxicity of anticancer candidate salinomycin and identification of its metabolites in rat cell cultures. Olejnik, M; Radko, L, 2018) | 0.48 |
| " There are many reports of its toxicity to animals but little is known about the potential adverse effects in humans." | ( Primary Human Hepatocytes, but Not HepG2 or Balb/c 3T3 Cells, Efficiently Metabolize Salinomycin and Are Resistant to Its Cytotoxicity. Olejnik, M; Posyniak, A; Radko, L, 2020) | 0.56 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "In compatibility with FA, AUC(0-t), Cmax and Tmax showed no significant difference with the single administration of TMP, but t(1/2) and MRT,, were obviously longer than the single administration." | ( [Effect of different compatibility of tetramethylpyrazine on its pharmacokinetics in vivo]. Chen, G; Feng, B; Xu, X; Zhang, J, 2012) | 0.38 |
| "The bioavailability and pharmacokinetic disposition of tiamulin in broiler chicken were investigated after administration through the crop, drinking water, and feed at 40 mg/kg body weight." | ( Pharmacokinetics and relative bioavailability of tiamulin in broiler chicken as influenced by different routes of administration. Preetha, SP; Ramesh, S; Sooraj Nair, V; Sriram, P; Vinothini, P, 2019) | 1.02 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " In a second challenge study, the dose rate of tiamulin combined with chlortetracycline was tested." | ( Efficacy of tiamulin alone or in combination with chlortetracycline against experimental Mycoplasma gallisepticum infection in chickens. Degussem, K; Depondt, W; Garmyn, A; Haesebrouck, F; Martel, A; Vereecken, M, 2017) | 1.09 |
The highest tiamulin serum concentrations (Cmax), the largest area under the curve (AUC0-->infinity), and the largest absorption rate constant (Ka) were obtained after administration via stomach tube followed in the respective order by the 2,000 mg/kg, 500mg/kg and 180 mg/ kg treatments.
| Excerpt | Reference | Relevance |
|---|---|---|
| " The highest tiamulin serum concentrations (Cmax), the largest area under the curve (AUC0-->infinity), the largest absorption rate constant (Ka), and the shortest time at which the maximum serum concentration occurred (tmax) were obtained after administration via stomach tube followed in the respective order by the 2,000 mg/kg, 500 mg/kg and 180 mg/kg treatments." | ( Influence of tiamulin concentration in feed on its bioavailability in piglets. Riond, JL; Schreiber, F; Wanner, M, 1993) | 1.02 |
| "The bioavailability and pharmacokinetic disposition of tiamulin in broiler chicken were investigated after administration through the crop, drinking water, and feed at 40 mg/kg body weight." | ( Pharmacokinetics and relative bioavailability of tiamulin in broiler chicken as influenced by different routes of administration. Preetha, SP; Ramesh, S; Sooraj Nair, V; Sriram, P; Vinothini, P, 2019) | 1.02 |
| "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 |
Dogs absorbed 86% of a single oral dose of tiamulin-3H. The disposition of the compound was similar after a single or multiple dosage regimen. 97 sows infected by Mycoplasma hyopneumoniae and Treponema hyodysenteriae were given 20 mg/kg bodyweight daily.
| Excerpt | Relevance | Reference |
|---|---|---|
| " Dogs absorbed 86% of a single oral dose of tiamulin-3H, and the disposition of the compound was similar after a single or multiple dosage regimen." | ( Metabolism of tritium- and carbon-14-labeled tiamulin in dogs, rats, and pigs. Battig, F; Czok, R; Dreyfuss, J; Egli, P; Nefzger-Biessels, M; Ross, JJ; Schmook, F; Schuster, I; Shaw, JM; Singhvi, SM, 1979) | 0.78 |
| " Prominent acute clinical signs of monensin toxicosis (hypermetria, hind limb ataxia, paresis, knuckling of hind limbs, and recumbency) developed by 2 to 6 hours after dosing in pigs given 15 or 25 mg of monensin/kg with tiamulin exposure, but not in pigs given the 15 or 25 mg of monensin/kg without tiamulin exposure." | ( Monensin toxicosis in swine: potentiation by tiamulin administration and ameliorative effect of treatment with selenium and/or vitamin E. Cook, JR; Runnels, LJ; Scheidt, AB; Van Vleet, JF, 1987) | 0.72 |
| "From 10 days before the expected date of farrowing onwards, 97 sows infected by Mycoplasma hyopneumoniae and Treponema hyodysenteriae were given tiamulin daily at a dosage of 20 mg/kg bodyweight via the feed." | ( Eradication of some infectious pig diseases by perinatal tiamulin treatment and early weaning. Antal, T; Mészáros, J; Stipkovits, L; Szabó, I; Veszely, P, 1985) | 0.71 |
| " Sows in five of the groups were dosed with high levels of tiamulin and trimethoprim-sulphonamide preparations from their entry into the farrowing house until their biggest piglets were weaned." | ( Medicated early weaning to obtain pigs free from pathogens endemic in the herd of origin. Alexander, TJ; Boon, G; Gush, AF; Lysons, RJ; Thornton, K, 1980) | 0.5 |
| " Twenty weaner pigs were challenged orally with a virulent inoculum of Lawsonia intracellularis strain LR189/5/83, a British isolate of the causative agent of porcine proliferative enteropathy, and seven control pigs were dosed with a buffer solution." | ( Treatment and prevention of porcine proliferative enteropathy with oral tiamulin. Carr, MM; McOrist, S; Miller, DJ; Shearn, MF; Smith, SH, ) | 0.36 |
| ") was investigated in dependence upon dosage and feeding method." | ( [Toxicity of the combination of salinomycin and tiamulin in swine]. Bollwahn, W; Büsing, S; Wendt, M, 1997) | 0.55 |
| " Tiamulin susceptibility testing methods appear to be accurate in their categorical classification for indicated species, and their availability will allow immediate testing of animal isolates to guide therapy via appropriate levels of dosing and to monitor the development of resistance for agents in this unique class." | ( Tiamulin activity against fastidious and nonfastidious veterinary and human bacterial isolates: initial development of in vitro susceptibility test methods. Jones, RN; Pfaller, MA; Rhomberg, PR; Walter, DH, 2002) | 2.67 |
| " To test the discriminative properties of the biomarkers, the dosage regimens were designed with an expected difference in therapeutic efficacy in favour of danofloxacin." | ( Putative biomarkers for evaluating antibiotic treatment: an experimental model of porcine Actinobacillus pleuropneumoniae infection. Angen, Ø; Friis, C; Lauritzen, B; Lykkesfeldt, J; Nielsen, JP; Skaanild, MT, 2003) | 0.32 |
| " The applied dosage was often lower than suggested in the literature." | ( [The use of macrolides, lincomycin and tiamulin as animal feed drugs for pigs in Schleswig-Holstein]. Bettin, U; Broll, S; Kietzmann, M; Kreienbrock, L, ) | 0.4 |
| " The control diet, containing only SAL at 60 mg/kg, was fed to all birds throughout the 35-d trial, including the period during the gaps between dosing (i." | ( Compatibility of a combination of tiamulin and chlortetracycline with salinomycin in feed during a pulsed medication program coadministration in broilers. Afrin, S; Burch, DG; Das, PM; Hassan, MM; Islam, KM; Kemppainen, BW; Klein, U; Valks, M, 2008) | 0.63 |
| " A clear dose-response effect was found for paromomycin." | ( Assessment of the antihistomonal effect of paromomycin and tiamulin. De Gussem, K; Landman, WJ; van der Heijden, HM, 2011) | 0.61 |
| Role | Description |
|---|---|
| antibacterial drug | A 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] | |
| Class | Description |
|---|---|
| carbotricyclic compound | A carbopolyclic compound comprising of three carbocyclic rings. |
| carboxylic ester | An ester of a carboxylic acid, R(1)C(=O)OR(2), where R(1) = H or organyl and R(2) = organyl. |
| cyclic ketone | |
| tertiary amino compound | A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups. |
| secondary alcohol | A secondary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has two other carbon atoms attached to it. |
| organic sulfide | Compounds having the structure RSR (R =/= H). Such compounds were once called thioethers. |
| tetracyclic diterpenoid | A diterpenoid with a tetracyclic skeleton. |
| semisynthetic derivative | Any organic molecular entity derived from a natural product by partial chemical synthesis. |
| [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) |
|---|---|---|---|---|---|---|---|
| TDP1 protein | Homo sapiens (human) | Potency | 5.2424 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 15.8489 | 0.0054 | 28.0263 | 1,258.9301 | AID1346985 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 18.9959 | 0.0002 | 29.3054 | 16,493.5996 | AID743069 |
| nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 11.2202 | 0.1000 | 9.1916 | 31.6228 | AID1346983 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 2.2387 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 25.1567 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 13.3332 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 19.9526 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 1.6000 | 0.0001 | 1.7536 | 10.0000 | AID1759746 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 30S ribosomal protein S6 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S7 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L15 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L10 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L11 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L7/L12 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L19 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L1 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L20 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L27 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L28 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L29 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L31 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L31 type B | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L32 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L33 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L34 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L35 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L36 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S10 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S11 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S12 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S13 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S16 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S18 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S19 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S20 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S2 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S3 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S4 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S5 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S8 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S9 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L13 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L14 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L16 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L23 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S15 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L17 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L21 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L30 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L6 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S14 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S17 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S1 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L18 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L2 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L3 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L24 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L4 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L22 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L5 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 30S ribosomal protein S21 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L25 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| 50S ribosomal protein L36 2 | Escherichia coli K-12 | Kd | 0.0363 | 0.0006 | 0.0231 | 0.0840 | AID1882851 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1638644 | Antimicrobial activity against Wolbachia wMel infected in Drosophila melanogaster LDW1 cells after 6 days by DAPI-based fluorescence in-situ hybridization assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis. |
| AID681470 | TP_TRANSPORTER: increase in Daunomycin intracellular accumulation (Daunomycin: 1.9 uM, Tiamulin: 2 uM) in AS30-D/COL10 cells, flow cytometry | 1998 | Biochemical pharmacology, Nov-01, Volume: 56, Issue:9 | In vitro and in vivo reversal of cancer cell multidrug resistance by the semi-synthetic antibiotic tiamulin. |
| AID583878 | Antibacterial activity against laboratory-derived Staphylococcus aureus ATCC 29213 harboring cfr-containing p42262 by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3. |
| AID1564968 | Antibacterial activity against methicillin-resistant Staphylococcus aureus infected in neutropenic thigh infection ICR/Swiss mouse model assessed reduction in colony forming unit in thigh at 20 mg/kg, iv administered 2 hrs post infection and measured at 2 | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives possessing acetamine phenyl linker. |
| AID1772463 | Bactericidal activity against Escherichia coli ATCC 25922 assessed as inhibition of bacterial growth measured after 96 hrs by broth dilution method | |||
| AID1772470 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as post antibiotic effect by measuring time required for increase in 1 log10 CFU/ml of bacteria at 2X MIC incubated for 2 hrs followed by compound washout and m | |||
| AID1741714 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as post antibacterial effect at 4 time of MIC concentration preincubated for 2 hrs followed by compound washout further incubated with fresh medium and measured | |||
| AID1889922 | Cytotoxicity against human HGC-27 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 04-01, Volume: 59 | Design, synthesis and antibacterial evaluation of pleuromutilin derivatives. |
| AID519076 | Antimicrobial activity against mutS-expressing Staphylococcus aureus RN4220 measured after 1 day of subculturing by agar dilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID1741702 | Antibacterial activity against Staphylococcus aureus 144 after 24 hrs by CLSI based broth micro dilution method | |||
| AID519091 | Antimicrobial activity against Staphylococcus aureus KM168 harboring Arg149Ser mutation in rplC gene by agar dilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID679736 | TP_TRANSPORTER: increase in Daunomycin intracellular accumulation (Daunomycin: 1.9 uM, Tiamulin: 2 uM) in CEM/VLB3.6 cells, flow cytometry | 1998 | Biochemical pharmacology, Nov-01, Volume: 56, Issue:9 | In vitro and in vivo reversal of cancer cell multidrug resistance by the semi-synthetic antibiotic tiamulin. |
| AID519089 | Antimicrobial activity against Staphylococcus aureus KM166-167 harboring Ser158Leu mutation in rplC gene by agar dilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID1889919 | Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 43300 at 4 times MIC and measured after 24 hrs by time kill curve assay relative to control | 2022 | Bioorganic & medicinal chemistry, 04-01, Volume: 59 | Design, synthesis and antibacterial evaluation of pleuromutilin derivatives. |
| AID560250 | Antibacterial activity against Staphylococcus aureus RN4220 harboring aadD and tet(L) gene by CLSI method | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Novel ABC transporter gene, vga(C), located on a multiresistance plasmid from a porcine methicillin-resistant Staphylococcus aureus ST398 strain. |
| AID684237 | Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis isolate cpu0347 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID1564960 | Antibacterial against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as post antibiotic effect time at 4 times MIC incubated for 2 hrs followed by compound washout and and then incubated for 20 hrs onto MH agar plate | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives possessing acetamine phenyl linker. |
| AID1867936 | Antibacterial activity against Escherichia coli assessed as inhibition of bacterial growth incubated for 24 hrs by microbroth two-fold dilution method | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Design, synthesis and antibacterial activity of novel pleuromutilin derivatives with thieno[2,3-d]pyrimidine substitution. |
| AID1436015 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 29213 at 160 ug/ml after 24 to 36 hrs by oxford cup assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID684233 | Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate cpu0887 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID323920 | Antibacterial activity against Staphylococcus aureus 2A1-7 fast2 with rplC D159Y and unmapped mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID1772461 | Bactericidal activity against Staphylococcus aureus AD3 assessed as inhibition of bacterial growth measured after 96 hrs by broth dilution method | |||
| AID1882841 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in ICR/Swiss mouse neuropathic thigh infection model assessed as log reduction in bacterial load in thigh at 20 mg/kg, iv administered as bolus injection measur | |||
| AID533665 | Antimicrobial activity against Staphylococcus aureus ATCC 29213 | 2008 | Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12 | Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus. |
| AID1704292 | Antibacterial activity against Staphylococcus aureus BNCC 337371 infected in Kunming mouse assessed as bacterial load in lung at 20 to 40 mg/kg, ip measured after 2 days by colony counting method (Rvb = 4.8 log10CFU/ml) | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation. |
| AID1436023 | Antibacterial activity against Escherichia coli CMCC (B) 44102 at 160 ug/ml after 24 to 36 hrs by oxford cup assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID684235 | Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate cpu3256 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID323903 | Antibacterial activity against wild type Staphylococcus aureus RN4220 | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID509632 | Antimicrobial activity against Staphylococcus aureus 25 transformant carrying plasmid pKKS25 and expressing erm(T), dfrKtet(L), tet(K), tet(M), mecA and blaZ genes by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Identification of a plasmid-borne resistance gene cluster comprising the resistance genes erm(T), dfrK, and tet(L) in a porcine methicillin-resistant Staphylococcus aureus ST398 strain. |
| AID1704282 | Antibacterial activity against Staphylococcus aureus BNCC 337371 measured after 18 to 24 hrs by microtiter dilution method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation. |
| AID323917 | Antibacterial activity against Staphylococcus aureus 2A1-1 fast1 with rplC D159Y and unmapped mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID1741699 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after 24 hrs by CLSI based broth micro dilution method | |||
| AID362374 | Binding affinity to Escherichia coli MRE600 ribosome assessed as protection against N1-cyclohexyl-N3-(2-morpholino)ethylcarbodiimide p-toluenesulfonate-induced modifications at nucleotide U2506 in peptidyl transferase center of 23S rRNA at 5 uM by chemica | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | A click chemistry approach to pleuromutilin conjugates with nucleosides or acyclic nucleoside derivatives and their binding to the bacterial ribosome. |
| AID1759744 | In vivo antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in ICR/Swiss mouse model of neutropenic thigh infection assessed as reduction in bacterial growth at 20 mg/kg, iv administered 2 hrs after infection and | 2021 | Bioorganic & medicinal chemistry, 05-15, Volume: 38 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives as potent anti-MRSA agents targeting the 50S ribosome. |
| AID1759748 | Binding affinity to Staphylococcus aureus ATCC 43300 50S ribosome assessed as association constant by SPR analysis | 2021 | Bioorganic & medicinal chemistry, 05-15, Volume: 38 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives as potent anti-MRSA agents targeting the 50S ribosome. |
| AID1436009 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 29213 after 24 to 48 hrs by agar dilution method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID1436031 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 29213 in iv dosed Balb/c mouse systemic infection model assessed as increase in mouse survival after 7 days | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID1638647 | Fraction unbound in mouse plasma at 1 uM | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis. |
| AID1882833 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as inhibition of bacterial growth incubated for 16 hrs by CLSI based broth microdilution method | |||
| AID1436011 | Antibacterial activity against Staphylococcus aureus CMCC (B) 26003 after 24 to 48 hrs by agar dilution method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID1436013 | Antibacterial activity against Escherichia coli CMCC (B) 44102 after 24 to 48 hrs by agar dilution method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID533660 | Antimicrobial activity against Staphylococcus aureus RN4220 harboring plasmid VGA | 2008 | Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12 | Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus. |
| AID509630 | Antimicrobial activity against Staphylococcus aureus RN4220 by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Identification of a plasmid-borne resistance gene cluster comprising the resistance genes erm(T), dfrK, and tet(L) in a porcine methicillin-resistant Staphylococcus aureus ST398 strain. |
| AID1889924 | Cytotoxicity against human MCF7 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 04-01, Volume: 59 | Design, synthesis and antibacterial evaluation of pleuromutilin derivatives. |
| AID1436014 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 29213 at 320 ug/ml after 24 to 36 hrs by oxford cup assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID678913 | TP_TRANSPORTER: increase in Daunomycin intracellular accumulation (Daunomycin: 1.9 uM, Tiamulin: 2 uM) in P388/ADR25 cells, flow cytometry | 1998 | Biochemical pharmacology, Nov-01, Volume: 56, Issue:9 | In vitro and in vivo reversal of cancer cell multidrug resistance by the semi-synthetic antibiotic tiamulin. |
| AID323916 | Antibacterial activity against Staphylococcus aureus 2A1-8 with rplC G152D, D159Y and unmapped mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID1759750 | Binding affinity to Staphylococcus aureus ATCC 43300 50S ribosome assessed as dissociation rate constant by SPR analysis | 2021 | Bioorganic & medicinal chemistry, 05-15, Volume: 38 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives as potent anti-MRSA agents targeting the 50S ribosome. |
| AID519084 | Antimicrobial activity against Escherichia coli KM75-84 harboring Gly153Arg mutation in rplC gene by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID684097 | Antibacterial activity against Escherichia coli AS19 after 24 hrs by microtitre plate reader | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5 | A click chemistry approach to pleuromutilin derivatives, part 2: conjugates with acyclic nucleosides and their ribosomal binding and antibacterial activity. |
| AID1436020 | Antibacterial activity against Bacillus subtilis CMCC (B) 63501 at 320 ug/ml after 24 to 36 hrs by oxford cup assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID684241 | Antibacterial activity against methicillin-resistant Staphylococcus epidermidis isolate cpu3889 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID583880 | Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-2 harboring ribosomal protein L3 Gly155Arg/Met169Leu mutant and cfr-containing p42262 by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3. |
| AID1564969 | Antibacterial activity against methicillin-resistant Staphylococcus aureus infected in systemic infection ICR mouse model assessed as animal survival rate at 30 mg/kg, iv relative to control | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives possessing acetamine phenyl linker. |
| AID1759741 | Antibacterial activity against Staphylococcus aureus AD3 assessed as inhibition of visible growth incubated for 24 hrs by CLSI protocol based broth microdilution method | 2021 | Bioorganic & medicinal chemistry, 05-15, Volume: 38 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives as potent anti-MRSA agents targeting the 50S ribosome. |
| AID583877 | Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-3 harboring ribosomal protein L3 deltaPhe127-His146 mutant by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3. |
| AID1377605 | Potentiation of doxorubicin-induced antitumor activity against mouse P388/DOX25 cells implanted in mouse assessed as increase in mouse survival at 1.6 mg/kg, ip | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Natural alkaloids as P-gp inhibitors for multidrug resistance reversal in cancer. |
| AID684239 | Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis isolate cpu1561 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID1741704 | Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 43300 preincubated 16 to 20 hrs followed by subculturing and measured after over night | |||
| AID519085 | Antimicrobial activity against Escherichia coli KM85-86 harboring Lys157Gln mutation in rplC gene by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID1759746 | Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate incubated for 5 mins followed by NADPH addition and measured after 5 mins by LC/MS/MS analysis | 2021 | Bioorganic & medicinal chemistry, 05-15, Volume: 38 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives as potent anti-MRSA agents targeting the 50S ribosome. |
| AID1428686 | Antibacterial activity against Enterococcus faecium ATCC 35667 after overnight incubation by broth dilution method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and antibacterial evaluation of novel pleuromutilin derivatives possessing piperazine linker. |
| AID1564958 | Antibacterial against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as post antibiotic effect time at 4 times MIC incubated for 1 hr followed by compound washout and then incubated for 20 hrs onto MH agar plate | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives possessing acetamine phenyl linker. |
| AID1759740 | Antibacterial activity against Staphylococcus aureus 144 assessed as inhibition of visible growth incubated for 24 hrs by CLSI protocol based broth microdilution method | 2021 | Bioorganic & medicinal chemistry, 05-15, Volume: 38 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives as potent anti-MRSA agents targeting the 50S ribosome. |
| AID542387 | Antimicrobial activity against Staphylococcus aureus RN4220 | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Methicillin-resistant and -susceptible Staphylococcus aureus strains of clonal lineages ST398 and ST9 from swine carry the multidrug resistance gene cfr. |
| AID533653 | Antimicrobial activity against Staphylococcus aureus IV20204009 harboring vgaAv positive Tn5406 transposon | 2008 | Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12 | Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus. |
| AID1436017 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 at 160 ug/ml after 24 to 36 hrs by oxford cup assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID520734 | Antimicrobial activity against methicillin-resistant Staphylococcus aureus CM05 by broth microdilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Transcriptional and translational control of the mlr operon, which confers resistance to seven classes of protein synthesis inhibitors. |
| AID1638645 | Intrinsic clearance in mouse liver S9 fraction | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis. |
| AID1867935 | Antibacterial activity against Streptococcus agalactiae assessed as inhibition of bacterial growth incubated for 24 hrs by microbroth two-fold dilution method | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Design, synthesis and antibacterial activity of novel pleuromutilin derivatives with thieno[2,3-d]pyrimidine substitution. |
| AID583705 | Antibacterial activity against clinical-derived Staphylococcus aureus isolate 42262 by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3. |
| AID583706 | Antibacterial activity against clinical-derived Staphylococcus aureus isolate harboring ribosomal protein L3 deltaSer145/His146Tyr mutant by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3. |
| AID1564957 | Antibacterial against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as post antibiotic effect time at 2 times MIC incubated for 1 hr followed by compound washout and then incubated for 20 hrs onto MH agar plate | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives possessing acetamine phenyl linker. |
| AID1772475 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as inhibition of bacterial growth measured after 8 passages at sub-MIC concentration incubated for 24 hrs by resistant development assay | |||
| AID562246 | Antibacterial activity against Staphylococcus epidermidis 1653059 harboring rplC G469A/C470G, L3 Ala157Arg and 23S rRNA G2447T mutant by CLSI broth microdilution assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | Mutations in ribosomal protein L3 are associated with oxazolidinone resistance in staphylococci of clinical origin. |
| AID1564948 | Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as bacterial growth inhibition incubated for 24 hrs by broth dilution method | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives possessing acetamine phenyl linker. |
| AID567567 | Antimicrobial activity against Bacillus sp. BS-01 expressing multiple resistance gene cfr and phenolic resistance gene fexA obtained from swine feces | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | First report of the multidrug resistance gene cfr and the phenicol resistance gene fexA in a Bacillus strain from swine feces. |
| AID1704280 | Antibacterial activity against Staphylococcus aureus ATCC 25923 measured after 18 to 24 hrs by microtiter dilution method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation. |
| AID519090 | Antimicrobial activity against Staphylococcus aureus RN4220 by agar dilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID1704298 | Antibacterial activity against Staphylococcus aureus BNCC 337371 infected in Kunming mouse assessed as reduction in infiltration of neutrophils cells at 20 to 40 mg/kg, ip measured after 2 days by H and E staining based light microscopic analysis | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation. |
| AID684096 | Binding affinity to Escherichia coli 23S rRNA U2585 assessed as degree of protection against CMCT at 50 uM by Chemical footprinting analysis relative to control | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5 | A click chemistry approach to pleuromutilin derivatives, part 2: conjugates with acyclic nucleosides and their ribosomal binding and antibacterial activity. |
| AID567569 | Antimicrobial activity against Staphylococcus aureus RN4220 | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | First report of the multidrug resistance gene cfr and the phenicol resistance gene fexA in a Bacillus strain from swine feces. |
| AID560247 | Antibacterial activity against Staphylococcus aureus RN4220 by CLSI method | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Novel ABC transporter gene, vga(C), located on a multiresistance plasmid from a porcine methicillin-resistant Staphylococcus aureus ST398 strain. |
| AID1882843 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in ICR/Swiss mouse systemic infection model assessed as survival rate at 30 mg/kg, iv administered as bolus injection 1 hr post infection measured twice daily a | |||
| AID684093 | Binding affinity to Escherichia coli 23S rRNA U2506 assessed as degree of protection against CMCT at 5 uM by Chemical footprinting analysis relative to control | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5 | A click chemistry approach to pleuromutilin derivatives, part 2: conjugates with acyclic nucleosides and their ribosomal binding and antibacterial activity. |
| AID1564950 | Antibacterial activity against Staphylococcus aureus AD3 assessed as bacterial growth inhibition incubated for 24 hrs by broth dilution method | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives possessing acetamine phenyl linker. |
| AID584993 | Antibacterial activity against Staphylococcus aureus XU21 by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | Identification and characterization of the multidrug resistance gene cfr in a Panton-Valentine leukocidin-positive sequence type 8 methicillin-resistant Staphylococcus aureus IVa (USA300) isolate. |
| AID1564955 | Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as reduction in colony forming unit at 4 times MIC incubated for 3 hrs followed by compound dilution with saline and then incubated for 20 hrs on MH agar plate b | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives possessing acetamine phenyl linker. |
| AID1759738 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as inhibition of visible growth incubated for 24 hrs by CLSI protocol based broth microdilution method | 2021 | Bioorganic & medicinal chemistry, 05-15, Volume: 38 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives as potent anti-MRSA agents targeting the 50S ribosome. |
| AID533661 | Antimicrobial activity against Staphylococcus aureus RN4220 harboring plasmid CU1 | 2008 | Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12 | Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus. |
| AID1882836 | Antibacterial activity against Staphylococcus aureus 144 assessed as inhibition of bacterial growth incubated for 16 hrs by CLSI based broth microdilution method | |||
| AID1889914 | Antibacterial activity against Staphylococcus epidermidis ATCC12228 assessed as inhibition of bacterial growth incubated for 18 hrs by two-fold serial dilution method | 2022 | Bioorganic & medicinal chemistry, 04-01, Volume: 59 | Design, synthesis and antibacterial evaluation of pleuromutilin derivatives. |
| AID1436027 | Bactericidal activity against Staphylococcus aureus CMCC (B) 26003 assessed as bacterial level at MIC after 1 to 24 hrs by time-kill assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID519082 | Antimicrobial activity against Escherichia coli KM69-73 harboring G2576U mutation in 23S rRNA by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID1882850 | Binding affinity to Staphylococcus aureus ATCC 43300 50S ribosomal subunit assessed as dissociation constant by surface plasmon resonance analysis | |||
| AID1867943 | Bactericidal activity against Staphylococcus aureus assessed as bacterial killing at 8 times MIC incubated up to 24 hrs by time kill assay | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Design, synthesis and antibacterial activity of novel pleuromutilin derivatives with thieno[2,3-d]pyrimidine substitution. |
| AID542385 | Antimicrobial activity against methicillin-resistant Staphylococcus aureus ST398 expressing cfr, fexA, erm(A), tet(M) and mecA genes | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Methicillin-resistant and -susceptible Staphylococcus aureus strains of clonal lineages ST398 and ST9 from swine carry the multidrug resistance gene cfr. |
| AID684243 | Antibacterial activity against methicillin-resistant Staphylococcus epidermidis isolate cpu2736 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID1882834 | Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as inhibition of bacterial growth incubated for 16 hrs by CLSI based broth microdilution method | |||
| AID1772454 | Antibacterial activity against Methycillin-resistant Staphylococcus aureus ATCC 43300 assessed as inhibition of bacterial growth measured after 24 hrs by broth dilution method | |||
| AID1704284 | Antibacterial activity against Streptococcus agalactiae measured after 18 to 24 hrs by microtiter dilution method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation. |
| AID1889920 | Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 04-01, Volume: 59 | Design, synthesis and antibacterial evaluation of pleuromutilin derivatives. |
| AID533654 | Antimicrobial activity against Staphylococcus aureus IV20205004 harboring vgaAv positive Tn5406 transposon | 2008 | Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12 | Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus. |
| AID1564959 | Antibacterial against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as post antibiotic effect time at 2 times MIC incubated for 2 hrs followed by compound washout and and then incubated for 20 hrs onto MH agar plate | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives possessing acetamine phenyl linker. |
| AID583707 | Antibacterial activity against clinical-derived Staphylococcus aureus isolate 51312 harboring ribosomal protein L3 deltaMet169-Gly174 mutant by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3. |
| AID323908 | Antibacterial activity against Staphylococcus aureus RN4220 with rplC G152D and D159Y mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID542389 | Antimicrobial activity against Staphylococcus aureus RN4220 transformed with Staphylococcus aureus ST9 plasmid pSCFS3 carrying cfr and fexA genes | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Methicillin-resistant and -susceptible Staphylococcus aureus strains of clonal lineages ST398 and ST9 from swine carry the multidrug resistance gene cfr. |
| AID1436016 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 at 320 ug/ml after 24 to 36 hrs by oxford cup assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID1867934 | Antibacterial activity against Staphylococcus aureus assessed as inhibition of bacterial growth incubated for 24 hrs by microbroth two-fold dilution method | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Design, synthesis and antibacterial activity of novel pleuromutilin derivatives with thieno[2,3-d]pyrimidine substitution. |
| AID1704287 | Antibacterial activity against Escherichia coli CICC 10389 measured after 18 to 24 hrs by microtiter dilution method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation. |
| AID684238 | Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis isolate cpu2089 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID1704299 | Antibacterial activity against Staphylococcus aureus BNCC 337371 infected in Kunming mouse assessed as reduction in local congestion in lung at 20 to 40 mg/kg, ip measured after 2 days by H and E staining based light microscopic analysis | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation. |
| AID1704285 | Antibacterial activity against Enterococcus faecalis measured after 18 to 24 hrs by microtiter dilution method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation. |
| AID520732 | Antimicrobial activity against Staphylococcus aureus RN4220 harboring plasmid LI50 by broth microdilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Transcriptional and translational control of the mlr operon, which confers resistance to seven classes of protein synthesis inhibitors. |
| AID684242 | Antibacterial activity against methicillin-resistant Staphylococcus epidermidis isolate cpu3569 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID323919 | Antibacterial activity against Staphylococcus aureus 2A1-7 fast1 with rplC D159Y and unmapped mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID533656 | Antimicrobial activity against Staphylococcus aureus IV20217033 harboring vgaA positive plasmid VGA | 2008 | Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12 | Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus. |
| AID519078 | Antimicrobial activity against tiamulin resistant Staphylococcus aureus 8325-4 after 1 day of subculturing by agar dilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID562249 | Antibacterial activity against Staphylococcus aureus NARSA NRS127 harboring rplC T433 to T435 and L3 Ser145 deletion mutant by CLSI broth microdilution assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | Mutations in ribosomal protein L3 are associated with oxazolidinone resistance in staphylococci of clinical origin. |
| AID533662 | Antimicrobial activity against Staphylococcus aureus RN4220 harboring vgaAv positive plasmid CU1 | 2008 | Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12 | Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus. |
| AID684098 | Antibacterial activity against Listeria innocua after 24 hrs by microtitre plate reader | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5 | A click chemistry approach to pleuromutilin derivatives, part 2: conjugates with acyclic nucleosides and their ribosomal binding and antibacterial activity. |
| AID1867937 | Antibacterial activity against Methicillin-resistant Staphylococcus aureus BNCC 337371 assessed as inhibition of bacterial growth incubated for 24 hrs by microbroth two-fold dilution method | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Design, synthesis and antibacterial activity of novel pleuromutilin derivatives with thieno[2,3-d]pyrimidine substitution. |
| AID1436024 | Bactericidal activity against Staphylococcus aureus CMCC (B) 26003 after 1 to 24 hrs by time-kill assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID1882849 | Binding affinity to Staphylococcus aureus ATCC 43300 50S ribosomal subunit assessed as association rate constant by surface plasmon resonance analysis | |||
| AID1772455 | Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as inhibition of bacterial growth measured after 24 hrs by broth dilution method | |||
| AID1772460 | Bactericidal activity against Staphylococcus aureus ATCC 29213 assessed as inhibition of bacterial growth measured after 96 hrs by broth dilution method | |||
| AID1428687 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in neutropenic mouse assessed as mouse survival rate at 40 mg/kg, iv administered 1 hr post infection relative to control | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and antibacterial evaluation of novel pleuromutilin derivatives possessing piperazine linker. |
| AID1741706 | Bactericidal activity against Staphylococcus aureus AD3 preincubated 16 to 20 hrs followed by subculturing and measured after over night | |||
| AID519088 | Antimicrobial activity against Staphylococcus aureus KM164-165 harboring Gly155Arg mutation in rplC gene by agar dilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID1377572 | Inhibition of P-gp ATPase activity in rat AS30-D/COL10 cell plasma membrane vesicles | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Natural alkaloids as P-gp inhibitors for multidrug resistance reversal in cancer. |
| AID1436018 | Antibacterial activity against Staphylococcus aureus CMCC (B) 26003 at 320 ug/ml after 24 to 36 hrs by oxford cup assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID1704290 | Antibacterial activity against Staphylococcus aureus BNCC 337371 infected in ip dosed Kunming mouse assessed as increase in mouse survival measured after 7 days | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation. |
| AID684236 | Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis isolate cpu0315 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID1889921 | Cytotoxicity against human U87 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 04-01, Volume: 59 | Design, synthesis and antibacterial evaluation of pleuromutilin derivatives. |
| AID1704289 | Bacteriostatic activity against Staphylococcus aureus BNCC 337371 assessed as reduction in bacterial load at 2 to 4 times MIC incubated for 8 hrs prior to 10 fold dilution followed by replating on MH agar plate and measured after 24 hrs by time-kill assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation. |
| AID1741700 | Antibacterial activity against Staphylococcus aureus ATCC 29213 after 24 hrs by CLSI based broth micro dilution method | |||
| AID1564953 | Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as reduction in colony forming unit at 4 times MIC incubated for 24 hrs followed by compound dilution with saline and then incubated for 20 hrs on MH agar plate | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives possessing acetamine phenyl linker. |
| AID560248 | Antibacterial activity against Staphylococcus aureus RN4220 harboring aadD, tet(L), dfrK and vga(C) gene by CLSI method | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Novel ABC transporter gene, vga(C), located on a multiresistance plasmid from a porcine methicillin-resistant Staphylococcus aureus ST398 strain. |
| AID1638643 | Antimicrobial activity against Wolbachia pipientis infected in Asian tiger mosquito C6/36 cells after 7 days by SYTO11 DNA dye-based confocal imaging analysis | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis. |
| AID519072 | Antimicrobial activity against tiamulin resistant Escherichia coli SQ110 by agar dilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID1436028 | Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 29213 assessed as bacterial level at MIC after 1 to 24 hrs by time-kill assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID1428685 | Antibacterial activity against Enterococcus faecalis ATCC 29212 after overnight incubation by broth dilution method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and antibacterial evaluation of novel pleuromutilin derivatives possessing piperazine linker. |
| AID323905 | Antibacterial activity against Staphylococcus aureus RN4220 with rplC G155R mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID1867933 | Antibacterial activity against Staphylococcus aureus assessed as diameter of the inhibition circle at 1 mg/ml incubated for 48 hrs | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Design, synthesis and antibacterial activity of novel pleuromutilin derivatives with thieno[2,3-d]pyrimidine substitution. |
| AID1741707 | Bactericidal activity against Staphylococcus aureus 144 preincubated 16 to 20 hrs followed by subculturing and measured after over night | |||
| AID1882837 | Antibacterial activity against Staphylococcus aureus SA17 assessed as inhibition of bacterial growth incubated for 16 hrs by CLSI based broth microdilution method | |||
| AID1772456 | Antibacterial activity against Staphylococcus aureus AD3 assessed as inhibition of bacterial growth measured after 24 hrs by broth dilution method | |||
| AID519095 | Antimicrobial activity against Staphylococcus aureus NRS121 clinical isolate harboring G2576U mutation in 23S rRNA by agar dilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID583875 | Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-1 harboring ribosomal protein L3 Gly155Arg mutant by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3. |
| AID1889911 | Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 assessed as inhibition of bacterial growth incubated for 18 hrs by two-fold serial dilution method | 2022 | Bioorganic & medicinal chemistry, 04-01, Volume: 59 | Design, synthesis and antibacterial evaluation of pleuromutilin derivatives. |
| AID533663 | Antimicrobial activity against Staphylococcus aureus RN1024 | 2008 | Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12 | Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus. |
| AID323914 | Antibacterial activity against Staphylococcus aureus 2A1-1 with rplC G152D, D159Y and unmapped mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID1436010 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 after 24 to 48 hrs by agar dilution method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID323915 | Antibacterial activity against Staphylococcus aureus 2A1-7 with rplC G152D, D159Y and unmapped mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID1704283 | Antibacterial activity against Streptococcus dysgalactiae measured after 18 to 24 hrs by microtiter dilution method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation. |
| AID362376 | Binding affinity to Escherichia coli MRE600 ribosome assessed as protection against N1-cyclohexyl-N3-(2-morpholino)ethylcarbodiimide p-toluenesulfonate-induced modifications at nucleotide U2585 in peptidyl transferase center of 23S rRNA at 5 uM by chemica | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | A click chemistry approach to pleuromutilin conjugates with nucleosides or acyclic nucleoside derivatives and their binding to the bacterial ribosome. |
| AID1436029 | Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 29213 after 1 to 24 hrs by time-kill assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID1759739 | Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as inhibition of visible growth incubated for 24 hrs by CLSI protocol based broth microdilution method | 2021 | Bioorganic & medicinal chemistry, 05-15, Volume: 38 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives as potent anti-MRSA agents targeting the 50S ribosome. |
| AID323913 | Antibacterial activity against Staphylococcus aureus RN4220 with rplC G152D, D159Y, G155R and A150T mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID583876 | Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-2 harboring ribosomal protein L3 Gly155Arg/Met169Leu mutant by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3. |
| AID519083 | Antimicrobial activity against Escherichia coli KM74 harboring U2500A mutation in 23S rRNA by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID323910 | Antibacterial activity against Staphylococcus aureus RN4220 with rplC G152D, D159Y and G144R mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID1436022 | Antibacterial activity against Escherichia coli CMCC (B) 44102 at 320 ug/ml after 24 to 36 hrs by oxford cup assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID1741705 | Bactericidal activity against Staphylococcus aureus ATCC 29213 preincubated 16 to 20 hrs followed by subculturing and measured after over night | |||
| AID1772457 | Antibacterial activity against Staphylococcus aureus 144 assessed as inhibition of bacterial growth measured after 24 hrs by broth dilution method | |||
| AID519087 | Antimicrobial activity against Escherichia coli KM89-94 harboring G2576U mutation in 23S rRNA by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID323907 | Antibacterial activity against Staphylococcus aureus RN4220 with rplC G152D mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID1882835 | Antibacterial activity against Staphylococcus aureus AD3 assessed as inhibition of bacterial growth incubated for 16 hrs by CLSI based broth microdilution method | |||
| AID684240 | Antibacterial activity against methicillin-resistant Staphylococcus epidermidis isolate cpu2623 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID1564947 | Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as reduction in colony forming unit at 4 times MIC incubated for 3 hrs followed by compound dilution with saline and then incubated for 20 hrs on MH agar plate b | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives possessing acetamine phenyl linker. |
| AID583881 | Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-3 harboring ribosomal protein L3 deltaPhe127-His146 mutant and cfr-containing p42262 by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3. |
| AID1889923 | Cytotoxicity against human HT-29 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 04-01, Volume: 59 | Design, synthesis and antibacterial evaluation of pleuromutilin derivatives. |
| AID584994 | Antibacterial activity against Staphylococcus aureus XU21-T1 harboring cfr-encoding conjugative pSCFS7 and fexA by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | Identification and characterization of the multidrug resistance gene cfr in a Panton-Valentine leukocidin-positive sequence type 8 methicillin-resistant Staphylococcus aureus IVa (USA300) isolate. |
| AID684231 | Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate cpu1344 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID323904 | Antibacterial activity against Staphylococcus aureus RN4220 with rplC D159Y mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID519074 | Antimicrobial activity against wild type Staphylococcus aureus RN4220 measured after 2 days of subculturing by agar dilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID1889913 | Antibacterial activity against Enterococcus faecium ATCC19434 assessed as inhibition of bacterial growth incubated for 18 hrs by two-fold serial dilution method | 2022 | Bioorganic & medicinal chemistry, 04-01, Volume: 59 | Design, synthesis and antibacterial evaluation of pleuromutilin derivatives. |
| AID1889912 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as inhibition of bacterial growth incubated for 18 hrs by two-fold serial dilution method | 2022 | Bioorganic & medicinal chemistry, 04-01, Volume: 59 | Design, synthesis and antibacterial evaluation of pleuromutilin derivatives. |
| AID520733 | Antimicrobial activity against Staphylococcus aureus RN4220 harboring plasmid MS2 by broth microdilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Transcriptional and translational control of the mlr operon, which confers resistance to seven classes of protein synthesis inhibitors. |
| AID1377606 | Inhibition of P-gp in rat AS30-D/COL10 cell plasma membrane vesicles assessed as reduction in [3H]VBL transport | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Natural alkaloids as P-gp inhibitors for multidrug resistance reversal in cancer. |
| AID519094 | Antimicrobial activity against Staphylococcus aureus NRS120 clinical isolate harboring G2576U mutation in 23S rRNA by agar dilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID1772459 | Bactericidal activity against Methycillin-resistant Staphylococcus aureus ATCC 43300 assessed as inhibition of bacterial growth measured after 96 hrs by broth dilution method | |||
| AID1882851 | Binding affinity to Staphylococcus aureus ATCC 43300 50S ribosomal subunit assessed as equilibrium dissociation constant by surface plasmon resonance analysis | |||
| AID519080 | Antimicrobial activity wild type Escherichia coli SQ110 by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID567568 | Antimicrobial activity against Staphylococcus aureus RN4220 harboring pBS-01multiple resistance gene cfr and phenolic resistance gene fexA obtained from swine feces | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | First report of the multidrug resistance gene cfr and the phenicol resistance gene fexA in a Bacillus strain from swine feces. |
| AID560249 | Antibacterial activity against Staphylococcus aureus RN4220 harboring tet(L), dfrK gene by CLSI method | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Novel ABC transporter gene, vga(C), located on a multiresistance plasmid from a porcine methicillin-resistant Staphylococcus aureus ST398 strain. |
| AID684232 | Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate cpu0446 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID362377 | Binding affinity to Escherichia coli MRE600 ribosome assessed as protection against N1-cyclohexyl-N3-(2-morpholino)ethylcarbodiimide p-toluenesulfonate-induced modifications at nucleotide U2585 in peptidyl transferase center of 23S rRNA at 50 uM by chemic | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | A click chemistry approach to pleuromutilin conjugates with nucleosides or acyclic nucleoside derivatives and their binding to the bacterial ribosome. |
| AID1428684 | Antibacterial activity against Staphylococcus aureus ATCC 29213 after overnight incubation by broth dilution method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and antibacterial evaluation of novel pleuromutilin derivatives possessing piperazine linker. |
| AID1772472 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in neutropenic CD1 mouse model of thigh infection assessed as reduction in bacterial colony forming unit in thigh at 20 mg/kg, iv qd measured after 24 hrs relat | |||
| AID1436025 | Bactericidal activity against Staphylococcus aureus CMCC (B) 26003 at 6 times MIC after 4 hrs by time-kill assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID519081 | Antimicrobial activity against Escherichia coli KM55-68 harboring G2576U mutation in 23S rRNA by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID1704288 | Bacteriostatic activity against Staphylococcus aureus BNCC 337371 assessed as reduction in bacterial load incubated for 2 to 24 hrs prior to 10 fold dilution followed by replating on MH agar plate and measured after 24 hrs by time-kill assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation. |
| AID1428683 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after overnight incubation by broth dilution method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and antibacterial evaluation of novel pleuromutilin derivatives possessing piperazine linker. |
| AID519092 | Antimicrobial activity against Staphylococcus aureus KM187+198 harboring G2576U mutation in 23S rRNA by agar dilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID684229 | Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate cpu0587 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID684094 | Binding affinity to Escherichia coli 23S rRNA U2506 assessed as degree of protection against CMCT at 50 uM by Chemical footprinting analysis relative to control | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5 | A click chemistry approach to pleuromutilin derivatives, part 2: conjugates with acyclic nucleosides and their ribosomal binding and antibacterial activity. |
| AID1741715 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in ICR/Swiss mouse model of neutropenic thigh infection assessed as reduction in bacterial load at 20 mg/kg, iv and measured after 24 hrs | |||
| AID1741713 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as post antibacterial effect at 2 time of MIC concentration preincubated for 2 hrs followed by compound washout further incubated with fresh medium and measured | |||
| AID323918 | Antibacterial activity against Staphylococcus aureus 2A1-1 fast2 with rplC D159Y and unmapped mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID1741716 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in ICR/Swiss mouse systemic infection model assessed as survival rate at 30 mg/kg, ip after 7 days relative to control | |||
| AID1772462 | Bactericidal activity against Staphylococcus aureus 144 assessed as inhibition of bacterial growth measured after 96 hrs by broth dilution method | |||
| AID1436012 | Antibacterial activity against Bacillus subtilis CMCC (B) 63501 after 24 to 48 hrs by agar dilution method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID323912 | Antibacterial activity against Staphylococcus aureus RN4220 with rplC G152D, D159Y, G155R and H134N mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID533658 | Antimicrobial activity against Staphylococcus aureus IHMA127277 harboring vgaAv positive Tn5406 transposon | 2008 | Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12 | Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus. |
| AID583879 | Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-1 harboring ribosomal protein L3 Gly155Arg mutant and cfr-containing p42262 by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3. |
| AID684095 | Binding affinity to Escherichia coli 23S rRNA U2585 assessed as degree of protection against CMCT at 5 uM by Chemical footprinting analysis relative to control | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5 | A click chemistry approach to pleuromutilin derivatives, part 2: conjugates with acyclic nucleosides and their ribosomal binding and antibacterial activity. |
| AID1704294 | Antibacterial activity against Staphylococcus aureus BNCC 337371 infected in Kunming mouse assessed as reduction in bacterial load in liver at 20 to 40 mg/kg, ip measured after 2 days by colony counting method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation. |
| AID533657 | Antimicrobial activity against Staphylococcus aureus IV20222009 harboring vgaAv positive Tn5406 transposon | 2008 | Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12 | Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus. |
| AID533659 | Antimicrobial activity against Staphylococcus aureus RN4220 | 2008 | Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12 | Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus. |
| AID562248 | Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 by CLSI broth microdilution assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | Mutations in ribosomal protein L3 are associated with oxazolidinone resistance in staphylococci of clinical origin. |
| AID684234 | Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate cpu1098 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID1772458 | Antibacterial activity against Escherichia coli ATCC 25922 assessed as inhibition of bacterial growth measured after 24 hrs by broth dilution method | |||
| AID1638648 | Apparent permeability of the compound in MDCK-MDR1 cells | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis. |
| AID533664 | Antimicrobial activity against Staphylococcus aureus RN1024-tms | 2008 | Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12 | Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus. |
| AID323906 | Antibacterial activity against Staphylococcus aureus RN4220 with rplC S158L mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID542388 | Antimicrobial activity against Staphylococcus aureus RN4220 transformed with Staphylococcus aureus ST398 plasmid pSCFS3 carrying cfr and fexA genes | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Methicillin-resistant and -susceptible Staphylococcus aureus strains of clonal lineages ST398 and ST9 from swine carry the multidrug resistance gene cfr. |
| AID362375 | Binding affinity to Escherichia coli MRE600 ribosome assessed as protection against N1-cyclohexyl-N3-(2-morpholino)ethylcarbodiimide p-toluenesulfonate-induced modifications at nucleotide U2506 in peptidyl transferase center of 23S rRNA at 50 uM by chemic | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | A click chemistry approach to pleuromutilin conjugates with nucleosides or acyclic nucleoside derivatives and their binding to the bacterial ribosome. |
| AID562247 | Antibacterial activity against methicillin-resistant Staphylococcus epidermidis ATCC 12228 by CLSI broth microdilution assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | Mutations in ribosomal protein L3 are associated with oxazolidinone resistance in staphylococci of clinical origin. |
| AID684230 | Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate cpu1044 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID1436021 | Antibacterial activity against Bacillus subtilis CMCC (B) 63501 at 160 ug/ml after 24 to 36 hrs by oxford cup assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID584996 | Antibacterial activity against methicillin-resistant Staphylococcus aureus M05/0060 harboring cfr-encoding conjugative pSCFS7 and fexA by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | Identification and characterization of the multidrug resistance gene cfr in a Panton-Valentine leukocidin-positive sequence type 8 methicillin-resistant Staphylococcus aureus IVa (USA300) isolate. |
| AID584995 | Antibacterial activity against pSCFS7-deficient methicillin-resistant Staphylococcus aureus M05/0060-C1 by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | Identification and characterization of the multidrug resistance gene cfr in a Panton-Valentine leukocidin-positive sequence type 8 methicillin-resistant Staphylococcus aureus IVa (USA300) isolate. |
| AID684267 | Antimicrobial activity against Mycoplasma by serial two fold dilution assay | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| AID1772471 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as post antibiotic effect by measuring time required for increase in 1 log10 CFU/ml of bacteria at 4X MIC incubated for 2 hrs followed by compound washout and m | |||
| AID583708 | Antibacterial activity against laboratory-derived Staphylococcus aureus ATCC 29213 by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3. |
| AID1564949 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as bacterial growth inhibition incubated for 24 hrs by broth dilution method | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives possessing acetamine phenyl linker. |
| AID1704281 | Antibacterial activity against Staphylococcus epidermidis ATCC 51625 measured after 18 to 24 hrs by microtiter dilution method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation. |
| AID323909 | Antibacterial activity against Staphylococcus aureus RN4220 with rplC G152D and G155R mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID1704286 | Antibacterial activity against Pasteurella multocida CVCC 1659 measured after 18 to 24 hrs by microtiter dilution method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation. |
| AID533655 | Antimicrobial activity against Staphylococcus aureus IV20217008 harboring vgaAv positive Tn5406 transposon | 2008 | Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12 | Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus. |
| AID519086 | Antimicrobial activity against Escherichia coli KM87-88 harboring Arg141Ser mutation in rplC gene by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID1759749 | Binding affinity to Staphylococcus aureus ATCC 43300 50S ribosome assessed as dissociation constant by SPR analysis | 2021 | Bioorganic & medicinal chemistry, 05-15, Volume: 38 | Design, synthesis and biological evaluation of novel pleuromutilin derivatives as potent anti-MRSA agents targeting the 50S ribosome. |
| AID519093 | Antimicrobial activity against Staphylococcus aureus NRS119 clinical isolate harboring G2576U mutation in 23S rRNA by agar dilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center. |
| AID542386 | Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ST9 expressing cfr, fexA and erm(C) genes | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Methicillin-resistant and -susceptible Staphylococcus aureus strains of clonal lineages ST398 and ST9 from swine carry the multidrug resistance gene cfr. |
| AID1436019 | Antibacterial activity against Staphylococcus aureus CMCC (B) 26003 at 160 ug/ml after 24 to 36 hrs by oxford cup assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID684099 | Antibacterial activity against Bacillus subtilis 168 after 12 hrs by microtitre plate reader | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5 | A click chemistry approach to pleuromutilin derivatives, part 2: conjugates with acyclic nucleosides and their ribosomal binding and antibacterial activity. |
| AID1436026 | Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 29213 at 6 times MIC after 4 hrs by time-kill assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety. |
| AID509631 | Antimicrobial activity against Staphylococcus aureus RN4220 transformant carrying plasmid pKKS25 and expressing erm(T), dfrK and tet(L) genes by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Identification of a plasmid-borne resistance gene cluster comprising the resistance genes erm(T), dfrK, and tet(L) in a porcine methicillin-resistant Staphylococcus aureus ST398 strain. |
| AID323911 | Antibacterial activity against Staphylococcus aureus RN4220 with rplC G152D, D159Y and G155R mutation | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin. |
| AID1741701 | Antibacterial activity against Staphylococcus aureus AD3 after 24 hrs by CLSI based broth micro dilution method | |||
| AID684228 | Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate cpu0211 after 18 to 20 hrs by agar dilution method | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies. |
| 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 | 62 (25.62) | 18.7374 |
| 1990's | 39 (16.12) | 18.2507 |
| 2000's | 61 (25.21) | 29.6817 |
| 2010's | 57 (23.55) | 24.3611 |
| 2020's | 23 (9.50) | 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 (46.34) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 15 (5.64%) | 5.53% |
| Reviews | 9 (3.38%) | 6.00% |
| Case Studies | 3 (1.13%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 239 (89.85%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||