Page last updated: 2024-12-11

platensimycin

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

Description

platensimycin: has antidiabetic and antisteatotic activities; a pentacyclic ketolide (structurally similar to adamantane) connected by an amide bond to 3-amino-2,4-dihydroxybenzoic acid; inhibits cellular lipid biosynthesis; discovered while screening compounds from Streptomyces platensis bacteria in a South African soil sample with S. aureus bacteria deficient in FabF protein; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

platensimycin : A monocarboxylic acid amide obtained by the formal condensation of the amino group of 3-amino-2,4-dihydroxybenzoic acid with the carboxy group of the oxatetracyclic cage component. It is an antibiotic isolated from Streptomyces platensis and exhibits inhibitory activity against fatty acid synthase. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID6857724
CHEMBL ID411278
CHEBI ID68236
MeSH IDM0498829

Synonyms (22)

Synonym
chebi:68236 ,
CHEMBL411278
PMN ,
platensimycin
(-)-platensimycin
DB08407
NCGC00183212-01
unii-q3dq78kofy
q3dq78kofy ,
835876-32-9
benzoic acid, 3-((3-((1s,3s,4s,5as,9s,9ar)-1,4,5,8,9,9a-hexahydro-3,9-dimethyl-8-oxo-3h-1,4:3,5a-dimethano-2-benzoxepin-9-yl)-1-oxopropyl)amino)-2,4-dihydroxy-
C20132
3-({3-[(1s,4as,6s,7s,9s,9ar)-1,6-dimethyl-2-oxo-1,2,5,6,7,8,9,9a-octahydro-6,9-epoxy-4a,7-methanobenzo[7]annulen-1-yl]propanoyl}amino)-2,4-dihydroxybenzoic acid
platensimycin [mi]
3-((3-((1s,3s,4s,5as,9s,9ar)-1,4,5,8,9,9a-hexahydro-3,9-dimethyl-8-oxo-3h-1,4:3,5a-dimethano-2-benzoxepin-9-yl)-1-oxopropyl)amino)-2,4-dihydroxybenzoic acid
platensimycin, (-)-
DTXSID80894888
Q423275
3-[3-[(1s,5s,6r,7s,9s,10s)-5,9-dimethyl-4-oxo-8-oxatetracyclo[7.2.1.17,10.01,6]tridec-2-en-5-yl]propanoylamino]-2,4-dihydroxybenzoic acid
CS-0093585
HY-127146
AKOS040754744

Research Excerpts

Overview

Platensimycin (PTM) is a potent FabB/FabF inhibitor, while its poor pharmacokinetics hampers the clinical development. It acts on bacterial fatty acid synthase and exhibits excellent antibacterial activity.

ExcerptReferenceRelevance
"Platensimycin (PTM) is a potent FabB/FabF inhibitor, while its poor pharmacokinetics hampers the clinical development."( Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
Deng, Y; Duan, Y; Huang, Y; Ji, X; Li, Y; Ren, N; Shen, B; Su, M; Wen, Z; Weng, X, 2019
)
1.52
"Platensimycin is a natural product isolated from a soil streptomycete, which contains an adamantane-like moiety extensively modified from a diterpenoid precursor."( Synthesis and biological evaluation of platensic alcohol as an adamantane surrogate in antitumor drug lead adaphostin.
Duan, Y; Huang, Y; Wen, Z; Xiong, Y, 2021
)
1.34
"Platensimycin (PTM) is a promising natural antibiotic lead that acts on bacterial fatty acid synthase and exhibits excellent antibacterial activity."( Platensimycin-berberine chloride co-amorphous drug system: Sustained release and prolonged half-life.
Bai, E; Chen, X; Duan, Y; Huang, Y; Li, D; Wang, Z; Zhang, H, 2022
)
2.89
"Platensimycin (PL) is a new promising antibiotic whose biosynthetic production is costly."( Membrane Affinity of Platensimycin and Its Dialkylamine Analogs.
Cember, A; Guo, M; Rowe, I; Sintim, HO; Sukharev, S; Yasmann, A, 2015
)
1.46
"Platensimycin (PTM) is a recently discovered broad-spectrum antibiotic produced by Streptomyces platensis. "( Antidiabetic and antisteatotic effects of the selective fatty acid synthase (FAS) inhibitor platensimycin in mouse models of diabetes.
Chung, CC; Ellsworth, KP; Karanam, BV; Lassman, ME; Lee, SH; Li, C; Miller, C; Myers, RW; Powles, M; Salituro, G; Singh, SB; Tota, MR; Wang, J; Wu, M; Zhang, BB, 2011
)
2.03
"Platensimycin (1a) is a novel broad spectrum Gram-positive antibiotic produced by Streptomyces platensis."( Isolation, structure, and absolute stereochemistry of platensimycin, a broad spectrum antibiotic discovered using an antisense differential sensitivity strategy.
Ball, RG; Basilio, A; Diez, MT; Genilloud, O; Herath, KB; Jayasuriya, H; Ondeyka, JG; Pelaez, F; Singh, SB; Tsou, NN; Vicente, F; Wang, J; Young, K; Zhang, C; Zink, DL, 2006
)
1.3
"Platensimycin is a natural product isolated from various strains of Streptomyces platensis which exhibits antimicrobial activity against Gram positive bacteria, including vancomycin- and linezolide-resistant species. "( Synthesis of platensimycin analogues and their antibiotic potency.
Bracher, F; Knorr, V; Krauss, J; Manhardt, V; Scheffels, S, 2008
)
2.16

Actions

ExcerptReferenceRelevance
"Platensimycin (1) displays antibacterial activity due to its inhibition of the elongation condensing enzyme (FabF), a novel mode of action that could potentially lead to a breakthrough in developing a new generation of antibiotics. "( Synthesis and biological evaluation of platensimycin analogs.
Chen, X; Colletti, SL; Ding, FX; Dorso, K; Ha, SN; Hammond, ML; Kodali, S; Maccoss, M; Parthasarathy, G; Shen, HC; Singh, SB; Soisson, SM; Tata, JR; Wang, J, 2009
)
2.06

Treatment

ExcerptReferenceRelevance
"Treatment with platensimycin eradicates Staphylococcus aureus infection in mice."( Platensimycin is a selective FabF inhibitor with potent antibiotic properties.
Allocco, J; Barrett, J; Bartizal, K; Basilio, A; Becker, JW; Colwell, L; Cully, D; Cummings, R; Dorso, K; Felcetto, T; Galgoci, A; Genilloud, O; Gill, C; Ha, S; Herath, K; Hermes, JD; Hernandez, L; Jayasuriya, H; Kodali, S; Lee, SH; Michael, B; Motyl, M; Ondeyka, J; Painter, R; Parthasarathy, G; Pelaez, F; Schmatz, D; Shoop, W; Silver, LL; Singh, SB; Soisson, SM; Tang, YS; Tormo, JR; Vicente, F; Wang, J; Young, K; Zhang, C, 2006
)
2.12
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
antimicrobial agentA substance that kills or slows the growth of microorganisms, including bacteria, viruses, fungi and protozoans.
EC 2.3.1.85 (fatty acid synthase) inhibitorAn EC 2.3.1.* (acyltransferase transferring other than amino-acyl group) inhibitor that interferes with the action of fatty acid synthase (EC 2.3.1.85), a multi-enzyme protein involved in fatty acid synthesis.
antibacterial agentA substance (or active part thereof) that kills or slows the growth of bacteria.
bacterial metaboliteAny prokaryotic metabolite produced during a metabolic reaction in bacteria.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (6)

ClassDescription
dihydroxybenzoic acidAny member of the class of hydroxybenzoic acids carrying two phenolic hydroxy groups on the benzene ring and its derivatives.
polycyclic cageA polycyclic compound having the shape of a cage.
cyclic etherAny ether in which the oxygen atom forms part of a ring.
cyclic ketone
aromatic amideAn amide in which the amide linkage is bonded directly to an aromatic system.
monocarboxylic acid amideA carboxamide derived from a monocarboxylic acid.
[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]

Bioassays (142)

Assay IDTitleYearJournalArticle
AID1563601Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3074 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430502Drug level in C57Bl/6 mouse plasma treated with platensimycin D1 at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430499Drug level in C57Bl/6 mouse urine at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1550810Antibacterial activity against Streptococcus pneumoniae
AID1563634Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 2962 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563633Inhibition of FabB/FabF in methicillin-sensitive Staphylococcus aureus 2955 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563620Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3140 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1350030Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate 1 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID1563631Inhibition of FabB/FabF in methicillin-sensitive Staphylococcus aureus 2952 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1350034Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 5 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID1563611Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3103 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563603Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3082 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563606Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3093 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430511Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by broth dilution method2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430476Volume of distribution in C57Bl/6 mouse at 3 mg/kg, iv administered as single dose by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430496Ratio of drug level in C57Bl/6 mouse adipose tissue to plasma at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1744573Binding affinity to His6-tagged Escherichia coli FabF C163Q mutant expressed in Escherichia coli BL21 (DE3) assessed as change in enthalpy measured after 200 sec by isothermal titration calorimetry2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID1563636Antibacterial activity against methicillin-resistant Staphylococcus aureus infected in C57BL/6J mouse model of peritonitis assessed as mouse survival at 10 mg/kg, ip dosed at 1 hr and 5 hrs post infection and measured for 7 days relative to control2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563614Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3108 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563621Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3150 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430512Antibacterial activity against Micrococcus luteus ATCC 9431 after 18 hrs by broth dilution method2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1563613Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3105 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430493Ratio of drug level in C57Bl/6 mouse lung to plasma at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1563604Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3086 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1412974Antibacterial activity against Staphylococcus aureus ATCC 29213 after 16 hrs by agar dilution method2018MedChemComm, May-01, Volume: 9, Issue:5
The semi-synthesis, biological evaluation and docking analysis of the oxime, hydrazine and hydrazide derivatives of platensimycin.
AID1744574Binding affinity to His6-tagged Escherichia coli FabF C163Q mutant expressed in Escherichia coli BL21 (DE3) assessed as change in entropy measured after 200 sec by isothermal titration calorimetry2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID1430513In vivo stability in C57Bl/6 mouse lung assessed as compound hydrolysis at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1550808Antibacterial activity against Staphylococcus aureus
AID1350033Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate 4 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID1744565Inhibition of Staphylococcus aureus FabH A81V/A111T mutant assessed as bacterial growth inhibition measured after 18 hrs by resazurin dye based broth dilution assay2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID1430490Drug uptake in C57Bl/6 mouse muscle at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430495Ratio of drug level in C57Bl/6 mouse muscle to plasma at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430518In vivo stability in C57Bl/6 mouse kidney assessed as compound hydrolysis by measuring platensic acid level at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis relative to platensimycin2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1434675Anti-bacterial activity against methicillin-susceptible Staphylococcus aureus CCARM 0027 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID1744564Antibacterial activity against methicillin resistant Staphylococcus aureus assessed as inhibition of bacterial growth measured after 16 hrs by agar plate dilution method2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID1744572Binding affinity to His6-tagged Escherichia coli FabF C163Q mutant expressed in Escherichia coli BL21 (DE3) assessed as stoichiometry ratio measured after 200 sec by isothermal titration calorimetry2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID1563619Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3116 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563605Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3090 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563632Inhibition of FabB/FabF in methicillin-sensitive Staphylococcus aureus 2954 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430460Elimination half life in C57Bl/6 mouse at 3 mg/kg, iv administered as single dose by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1563609Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3097 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430505Drug metabolism in mouse hepatic microsomes assessed as amide hydrolysis-mediated platensic acid formation at 1 uM up to 60 mins in presence of NADPH by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1563582Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus assessed as antibacterial activity at 5 ug/disk after 18 hrs by agar disk diffusion method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430504Intrinsic clearance in mouse hepatic microsomes at 1 uM up to 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1563610Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3100 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430471AUC (0 to 8 hrs) in C57Bl/6 mouse at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1412976Antibacterial activity against methicillin-resistant Staphylococcus aureus after 16 hrs by agar dilution method2018MedChemComm, May-01, Volume: 9, Issue:5
The semi-synthesis, biological evaluation and docking analysis of the oxime, hydrazine and hydrazide derivatives of platensimycin.
AID1563595Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 2984 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563630Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3196 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1350038Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 9 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID1324787Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 measured after 18 hrs by broth dilution method2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Antibacterial sulfur-containing platensimycin and platencin congeners from Streptomyces platensis SB12029.
AID1563590Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 2959 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563593Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 2978 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430488Drug uptake in C57Bl/6 mouse lung at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1744555Antibacterial activity against Enterococcus faecalis ATCC 29212 assessed as inhibition of bacterial growth measured after 16 hrs by agar plate dilution method2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID1744571Binding affinity to His6-tagged Escherichia coli FabF C163Q mutant expressed in Escherichia coli BL21 (DE3) assessed as binding constant measured after 200 sec by isothermal titration calorimetry2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID1350029Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID1563626Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3181 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1350036Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 7 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID1563635Inhibition of FabB/FabF in methicillin-sensitive Staphylococcus aureus 2956 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430515In vivo stability in C57Bl/6 mouse adipose tissue assessed as compound hydrolysis at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1350031Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate 2 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID1430524In vivo stability in C57Bl/6 mouse brain assessed as compound hydrolysis at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1434678Anti-bacterial activity against methicillin-susceptible Staphylococcus aureus CCARM 3640 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID1744562Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as inhibition of bacterial growth measured after 16 hrs by agar plate dilution method2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID1430475Observed clearance in C57Bl/6 mouse at 3 mg/kg, iv administered as single dose by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1434677Anti-bacterial activity against methicillin-susceptible Staphylococcus aureus CCARM 0205 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID1430516In vivo stability in C57Bl/6 mouse plasma assessed as compound hydrolysis by measuring platensic acid level at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis relative to platensimycin2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430486Drug uptake in C57Bl/6 mouse plasma at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430466Cmax in C57Bl/6 mouse at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1563599Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3065 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430485Plasma concentration in C57Bl/6 mouse at 3 mg/kg, iv administered as single dose measured after 2 hrs by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430483Oral bioavailability in C57Bl/6 mouse at 10 mg/kg administered as single dose via gavage by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1563624Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3161 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563615Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3110 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1744563Antibacterial activity against methicillin sensitive Staphylococcus aureus assessed as inhibition of bacterial growth measured after 16 hrs by agar plate dilution method2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID1430506Drug metabolism in mouse hepatic microsomes assessed as amide hydrolysis-mediated platensic acid formation at 1 uM up to 60 mins in absence of NADPH by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1550809Antibacterial activity against Enterococcus faecium
AID1563627Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3182 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563586Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563589Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 2957 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1434679Anti-bacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3089 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID1563594Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 2980 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1768533Antibacterial activity against methicillin-resistant Staphylococcus aureus2021Bioorganic & medicinal chemistry letters, 09-15, Volume: 48Synthesis and biological evaluation of platensic alcohol as an adamantane surrogate in antitumor drug lead adaphostin.
AID1563592Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 2976 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1350032Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate 3 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID1744575Binding affinity to His6-tagged Escherichia coli FabF C163Q mutant expressed in Escherichia coli BL21 (DE3) assessed Gibbs free energy change measured after 200 sec by isothermal titration calorimetry2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID1430498Apparent permeability by PAMPA2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1412975Antibacterial activity against methicillin-sensitive Staphylococcus aureus after 16 hrs by agar dilution method2018MedChemComm, May-01, Volume: 9, Issue:5
The semi-synthesis, biological evaluation and docking analysis of the oxime, hydrazine and hydrazide derivatives of platensimycin.
AID1434682Anti-bacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3635 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID1430514In vivo stability in C57Bl/6 mouse muscle assessed as compound hydrolysis at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430487Drug uptake in C57Bl/6 mouse liver at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430465Cmax in C57Bl/6 mouse at 3 mg/kg, iv administered as single dose by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430497Drug uptake in C57Bl/6 mouse brain at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430521In vivo stability in C57Bl/6 mouse liver assessed as compound hydrolysis at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430470AUC (0 to 8 hrs) in C57Bl/6 mouse at 3 mg/kg, iv administered as single dose by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1744568Antibacterial activity against Escherichia coli harboring delta tolC mutant assessed as inhibition of bacterial growth measured after 16 hrs by agar plate dilution method2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID1434681Anti-bacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3634 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID1563597Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3046 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430523In vivo stability in C57Bl/6 mouse urine assessed as compound hydrolysis at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1563607Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3094 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563602Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3079 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1434676Anti-bacterial activity against methicillin-susceptible Staphylococcus aureus CCARM 0204 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID1563596Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 2985 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430461Elimination half life in C57Bl/6 mouse at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1563622Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3156 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1350028Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 11 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID1563591Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 2968 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1744566Inhibition of Staphylococcus aureus FabH A81V mutant assessed as bacterial growth inhibition measured after 18 hrs by resazurin dye based broth dilution assay2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID1563588Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 2953 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430520In vivo stability in C57Bl/6 mouse plasma assessed as compound hydrolysis at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1563587Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 2951 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1350037Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 8 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID1563628Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3188 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1434680Anti-bacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3090 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID1563625Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3163 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563585Inhibition of FabB/FabF in methicillin-sensitive Staphylococcus aureus assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1324788Antibacterial activity against Micrococcus luteus ATCC 9431 measured after 18 hrs by broth dilution method2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Antibacterial sulfur-containing platensimycin and platencin congeners from Streptomyces platensis SB12029.
AID1563608Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3095 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430517In vivo stability in C57Bl/6 mouse liver assessed as compound hydrolysis by measuring platensic acid level at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis relative to platensimycin2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1563612Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3104 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430500Ratio of drug level in C57Bl/6 mouse urine to plasma at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1563629Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3193 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563584Inhibition of FabB/FabF in Staphylococcus aureus ATCC 29213 assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563616Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3111 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1350039Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 10 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID1430491Drug uptake in C57Bl/6 mouse adipose tissue at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430492Ratio of drug level in C57Bl/6 mouse liver to plasma at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1563598Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3056 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563623Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3158 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430510Drug metabolism in mouse hepatic microsomes assessed as glucuronidation of carboxylic acid at 1 uM up to 60 mins in absence of NADPH by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1350035Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 6 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID1430494Ratio of drug level in C57Bl/6 mouse kidney to plasma at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1563618Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3114 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430509Drug metabolism in mouse hepatic microsomes assessed as hydroxylation at 1 uM up to 60 mins in absence of NADPH by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430484Plasma concentration in C57Bl/6 mouse at 3 mg/kg, iv administered as single dose measured after 5 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430489Drug uptake in C57Bl/6 mouse kidney at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1563600Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3071 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1563617Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus 3112 clinical isolate assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1430522In vivo stability in C57Bl/6 mouse kidney assessed as compound hydrolysis at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1430519In vivo stability in C57Bl/6 mouse urine assessed as compound hydrolysis by measuring platensic acid level at 10 mg/kg, iv administered as single dose measured after 60 mins by LC-MS/MS analysis relative to platensimycin2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
AID1744567Antibacterial activity against methicillin resistant Staphylococcus aureus assessed as inhibition of bacterial growth measured after 18 hrs in presence of 10% human serum by resazurin dye based broth dilution assay2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (112)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's45 (40.18)29.6817
2010's58 (51.79)24.3611
2020's9 (8.04)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.50

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index29.50 (24.57)
Research Supply Index4.73 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index39.34 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.50)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews16 (14.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other96 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]