Page last updated: 2024-11-13

pc190723

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Description

PC190723: Antibacterial; an inhibitor of FtsZ with potent and selective anti-staphylococcal activity including methicillin- and multi-drug-resistant Staphylococcus aureus; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID25016417
CHEMBL ID511201
SCHEMBL ID2706605
MeSH IDM0525456

Synonyms (21)

Synonym
CHEMBL511201 ,
3-[(6-chloro[1,3]thiazolo[5,4-b]pyridin-2-yl)methoxy]-2,6-difluorobenzamide
9pc ,
951120-33-5
pc-190723
benzamide, 3-((6-chlorothiazolo(5,4-b)pyridin-2-yl)methoxy)-2,6-difluoro-
3-((6-chlorothiazolo(5,4-b)pyridin-2-yl)methoxy)-2,6-difluorobenzamide
7V5K32W934 ,
SCHEMBL2706605
pc 190723
pc190723
unii-7v5k32w934
3-((6-chlorothiazolo[5,4-b]pyridin-2-yl)methoxy)-2,6-difluorobenzamide
bdbm50079356
DTXSID80648429
3-[(6-chlorothiazolo[5,4-b]pyridin-2-yl)methoxy]-2,6-difluorobenzamide
3-[(6-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl)methoxy]-2,6-difluorobenzamide
Q27268896
3-({6-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}methoxy)-2,6-difluorobenzamide
CS-0498290
HY-146331

Research Excerpts

Overview

PC190723 is an effective bactericidal cell division inhibitor that targets FtsZ in the pathogen Staphylococcus aureus. It does not affect Escherichia coli cells, which apparently binds to a zone equivalent to the binding site of the antitumor drug taxol in tubulin.

ExcerptReferenceRelevance
"PC190723 is a fluoride-containing benzamide compound developed as a FtsZ inhibitor that selectively inhibits growth of multidrug resistant Gram-positive bacteria."( RfiA, a novel PAP2 domain-containing polytopic membrane protein that confers resistance to the FtsZ inhibitor PC190723.
An, L; Chen, T; Chen, X; Dyson, P; Facey, P; Ju, F; Li, S; Liu, G; Mullins, JG; Ren, C; Xiao, J; Zhang, B, 2015
)
1.35
"PC190723 is an effective bactericidal cell division inhibitor that targets FtsZ in the pathogen Staphylococcus aureus and Bacillus subtilis and does not affect Escherichia coli cells, which apparently binds to a zone equivalent to the binding site of the antitumor drug taxol in tubulin (Haydon, D."( The antibacterial cell division inhibitor PC190723 is an FtsZ polymer-stabilizing agent that induces filament assembly and condensation.
Alonso, D; Andreu, JM; Huecas, S; Llorca, O; Lopez-Rodriguez, ML; Martín-Galiano, AJ; Núñez-Ramírez, R; Ruiz-Avila, LB; Schaffner-Barbero, C, 2010
)
1.35

Pharmacokinetics

The clinical development of FtsZ-targeting benzamide compounds has been limited by poor drug-like and pharmacokinetic properties. In staphylococcal growth media, TXY541 converts to PC190723 with a half-life of approximately 8h.

ExcerptReferenceRelevance
" In staphylococcal growth media, TXY541 converts to PC190723 with a half-life of approximately 8h."( Pharmacokinetics and in vivo antistaphylococcal efficacy of TXY541, a 1-methylpiperidine-4-carboxamide prodrug of PC190723.
Kaul, M; LaVoie, EJ; Mark, L; Parhi, AK; Pilch, DS; Zhang, Y, 2013
)
0.85
"The clinical development of FtsZ-targeting benzamide compounds like PC190723 has been limited by poor drug-like and pharmacokinetic properties."( TXA709, an FtsZ-Targeting Benzamide Prodrug with Improved Pharmacokinetics and Enhanced In Vivo Efficacy against Methicillin-Resistant Staphylococcus aureus.
Kaul, M; LaVoie, EJ; Lyu, YL; Mark, L; Parhi, AK; Pawlak, J; Pilch, DS; Saravolatz, LD; Saravolatz, S; Weinstein, MP; Zhang, Y, 2015
)
0.65

Bioavailability

ExcerptReferenceRelevance
" In addition, TXY436 was found to be orally bioavailable and associated with significant extravascular distribution."( An FtsZ-targeting prodrug with oral antistaphylococcal efficacy in vivo.
Kaul, M; Lavoie, EJ; Mark, L; Parhi, AK; Pilch, DS; Zhang, Y, 2013
)
0.39
"56h and an oral bioavailability of 29."( Pharmacokinetics and in vivo antistaphylococcal efficacy of TXY541, a 1-methylpiperidine-4-carboxamide prodrug of PC190723.
Kaul, M; LaVoie, EJ; Mark, L; Parhi, AK; Pilch, DS; Zhang, Y, 2013
)
0.6
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cell division protein FtsZBacillus subtilisKd0.10000.10000.10000.1000AID1811677
Cell division protein FtsZStaphylococcus aureusEC50 (µMol)4.00004.00004.00004.0000AID1205864
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cell division protein FtsZBacillus subtilisActivity0.10000.10000.10000.1000AID1811661
Cell division protein FtsZStaphylococcus aureusActivity0.10000.10000.10000.1000AID1628127
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (144)

Assay IDTitleYearJournalArticle
AID1414194Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID1443332Inhibition of FtsZ in Mycobacterium smegmatis ATCC 607 assessed as growth inhibition at 100 ug per disc after 18 to 24 hrs by paper disc agar diffusion assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Synthesis and antibacterial activity of 3-benzylamide derivatives as FtsZ inhibitors.
AID394518Antibacterial activity against Bacillus subtilis by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1534161Inhibition of Staphylococcus aureus N-terminal 6His-tagged FtsZ polymerization expressed in Escherichia coli BL21 (DE3) at 100 uM relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163Boosting the efficacy of anti-MRSA β-lactam antibiotics via an easily accessible, non-cytotoxic and orally bioavailable FtsZ inhibitor.
AID394537Antibacterial activity against Staphylococcus aureus bearing FtsZ G196A mutant by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1326327Antibacterial activity against methicillin-resistant Staphylococcus aureus2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Recent advances in the discovery and development of antibacterial agents targeting the cell-division protein FtsZ.
AID1533843Antibacterial activity against Escherichia coli ATCC 25922 by broth microdilution assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Boosting the efficacy of anti-MRSA β-lactam antibiotics via an easily accessible, non-cytotoxic and orally bioavailable FtsZ inhibitor.
AID394546Antibacterial activity against Staphylococcus aureus Smith ATCC 19636 in CD1 mouse septicemia model assessed as survival at 30 mg/kg, sc after 7 days relative to control2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID394520Antibacterial activity against methicillin-resistant Staphylococcus aureus by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1850146Antibacterial activity against methicillin-resistant Staphylococcus aureus BAA 1720 assessed as inhibition of bacterial growth incubated for 18 hrs by CLSI protocol based two fold serial dilution method2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1591545Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID394532Antibacterial activity against Streptococcus pneumoniae by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1850161Inhibition of GFP-tagged FtsZ in Bacillus subtilis 168 assessed as inhibition of z-ring formation at 0.125 ug/ml incubated for 4 hrs by FM 5-96 dye based super-resolution microscopy2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1060729Antibacterial activity against Staphylococcus aureus ATCC 29213 by broth microdilution method2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Design, synthesis and structure-activity relationships of substituted oxazole-benzamide antibacterial inhibitors of FtsZ.
AID1591560Bactericidal activity against Staphylococcus aureus ATCC 25923 assessed as 3 log reduction in number of colony forming units incubated for 24 hrs followed by aliquots transfer to tryptic soy agar and grown for 24 hrs2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1850151Synergistic antibacterial activity against methicillin-resistant Staphylococcus aureus BAA 41 assessed as inhibition of bacterial growth incubated for 18 hrs in presence of methicillin by checkerboard assay2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1850155Synergistic antibacterial activity against methicillin-resistant Staphylococcus aureus BAA 41 assessed as FICI incubated for 18 hrs in presence of methicillin by checkerboard assay2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID394547Antibacterial activity against Staphylococcus aureus Smith ATCC 19636 in CD1 mouse septicemia model assessed as survival at 30 mg/kg, iv after 7 days relative to control2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1060728Inhibition of Staphylococcus aureus ATCC 29213 FtsZ-mediated cell division phenotype2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Design, synthesis and structure-activity relationships of substituted oxazole-benzamide antibacterial inhibitors of FtsZ.
AID1850171Inhibition of Staphylococcus aureus FtsZ polymerization assessed as increase in GTPase activity at 16 ug/ml incubated for 40 mins in presence of GTP by malachite green phosphate assay2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID394526Antibacterial activity against Staphylococcus saprophyticus by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1811667Antimicrobial activity against Bacillus subtilis 168 assessed as inhibition of bacterial growth by CLSI based broth macrodilution method2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Targeting the FtsZ Allosteric Binding Site with a Novel Fluorescence Polarization Screen, Cytological and Structural Approaches for Antibacterial Discovery.
AID1811666Antimicrobial activity against methicillin resistant Staphylococcus aureus Mu50 assessed as inhibition of bacterial growth by CLSI based broth macrodilution method2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Targeting the FtsZ Allosteric Binding Site with a Novel Fluorescence Polarization Screen, Cytological and Structural Approaches for Antibacterial Discovery.
AID1591562Bactericidal activity against penicillin-resistant Staphylococcus aureus clinical isolate assessed as 3 log reduction in number of colony forming units incubated for 24 hrs followed by aliquots transfer to tryptic soy agar and grown for 24 hrs2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1534182Synergistic antibacterial activity against Staphylococcus aureus ATCC BAA-41 at 1 to 16 times MIC in presence of methicillin after 21 hrs by time kill assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Boosting the efficacy of anti-MRSA β-lactam antibiotics via an easily accessible, non-cytotoxic and orally bioavailable FtsZ inhibitor.
AID394548Antibacterial activity against Staphylococcus aureus Smith ATCC 19636 in sc dosed CD1 mouse septicemia model assessed as survival after 7 days2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1677802Antibacterial activity against Pseudomonas aeruginosa ATCC27853 incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID1201502Antimicrobial activity against Staphylococcus2015European journal of medicinal chemistry, May-05, Volume: 95Advances in the discovery of novel antimicrobials targeting the assembly of bacterial cell division protein FtsZ.
AID1591540Antibacterial activity against Staphylococcus aureus ATCC 25923 incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1811663Binding affinity to Staphylococcus aureus FtsZ polymer assessed as dissociation constant by fluorescence anisotropy analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Targeting the FtsZ Allosteric Binding Site with a Novel Fluorescence Polarization Screen, Cytological and Structural Approaches for Antibacterial Discovery.
AID1850166Bactericidal activity against methicillin-resistant Staphylococcus aureus BAA 41 assessed as inhibition of bacterial growth at 8 ug/ml incubated for 24 hrs by time-kill assay2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID394533Antifungal activity against Saccharomyces cerevisiae by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID394519Antibacterial activity against Staphylococcus aureus by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID394550Antibacterial activity against Staphylococcus aureus Smith ATCC 19636 in ip dosed CD1 mouse septicemia model assessed as survival administered 1 hr postinfection measured after 7 days2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1591561Bactericidal activity against Staphylococcus aureus ATCC 43300 assessed as 3 log reduction in number of colony forming units incubated for 24 hrs followed by aliquots transfer to tryptic soy agar and grown for 24 hrs2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1850159Antibacterial activity against Bacillus subtilis 168 assessed as cell length at 0.5 ug/ml incubated for 4 hrs by phase-contrast microscopy2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1677804Antibacterial activity against Staphylococcus aureus clinical isolate incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID1591544Antibacterial activity against Escherichia coli ATCC 25922 incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1374407Antibacterial activity against Escherichia coli ATCC 25922 after 24 hrs by broth microdilution method2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Substitution of terminal amide with 1H-1,2,3-triazole: Identification of unexpected class of potent antibacterial agents.
AID394555Inhibition of cell division in Staphylococcus aureus ATCC 29213 assessed as enlargement of cells at 2 ug/ml within 2 hrs by phase contrast microscopy2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1677809Antibacterial activity against Bacillus subtilis ATCC9372 incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID1414189Antibacterial activity against Bacillus pumilus CMCC63202 after 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID1443327Inhibition of FtsZ in Staphylococcus aureus ATCC 6538P assessed as ratio of diameter of zone inhibition of test compound to diameter of zone inhibition of cephaloridine at 100 ug per disc after 18 to 24 hrs by paper disc agar diffusion assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Synthesis and antibacterial activity of 3-benzylamide derivatives as FtsZ inhibitors.
AID1850141Antibacterial activity against methicillin-resistant Staphylococcus aureus BAA 41 assessed as inhibition of bacterial growth incubated for 18 hrs by CLSI protocol based two fold serial dilution method2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1534168Inhibition of Staphylococcus aureus N-terminal 6His-tagged FtsZ GTPase expressed in Escherichia coli BL21 (DE3) at 50 uM relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163Boosting the efficacy of anti-MRSA β-lactam antibiotics via an easily accessible, non-cytotoxic and orally bioavailable FtsZ inhibitor.
AID394523Antibacterial activity against Staphylococcus haemolyticus by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1811661Binding affinity to Bacillus subtilis FtsZ polymer assessed as dissociation constant by fluorescence anisotropy analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Targeting the FtsZ Allosteric Binding Site with a Novel Fluorescence Polarization Screen, Cytological and Structural Approaches for Antibacterial Discovery.
AID1628127Activation of Staphylococcus aureus FtsZ assessed as increase in GTPase activity by malachite green assay2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
Targeting the Bacterial Division Protein FtsZ.
AID1326326Antibacterial activity against Bacillus subtilis2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Recent advances in the discovery and development of antibacterial agents targeting the cell-division protein FtsZ.
AID1205864Activation of Staphylococcus aureus FtsZ GTPase activity2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Synthesis and Evaluation of Quinazolines as Inhibitors of the Bacterial Cell Division Protein FtsZ.
AID1534180Antibacterial activity against Staphylococcus aureus ATCC BAA-41 at 116 times MIC after 24 hrs by time kill assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Boosting the efficacy of anti-MRSA β-lactam antibiotics via an easily accessible, non-cytotoxic and orally bioavailable FtsZ inhibitor.
AID394528Antibacterial activity against Enterococcus faecalis by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1414190Antibacterial activity against Staphylococcus aureus ATCC 25923 after 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID394542Antibacterial activity against Bacillus subtilis bearing FtsZ G196A mutant by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1591543Antibacterial activity against Staphylococcus aureus clinical isolate incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1677805Antibacterial activity against penicillin-resistant Staphylococcus aureus incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID394551Inhibition of Staphylococcus aureus FtsZ GTPase activity2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID394554Inhibition of cell division in Staphylococcus aureus ATCC 29213 assessed as enlargement of cells at 2 ug/ml by phase contrast microscopy2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1443331Inhibition of FtsZ in Bacillus subtilis ATCC 6633 assessed as growth inhibition at 100 ug per disc after 18 to 24 hrs by paper disc agar diffusion assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Synthesis and antibacterial activity of 3-benzylamide derivatives as FtsZ inhibitors.
AID1414192Antibacterial activity against clinical isolate of penicillin-resistant Staphylococcus aureus after 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID394560Enhancement of bovine brain tubulin polymerization at 64 ug/ml2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID394522Antibacterial activity against Staphylococcus epidermidis by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID394539Antibacterial activity against Staphylococcus aureus bearing FtsZ N263K mutant by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1850164Bactericidal activity against methicillin-resistant Staphylococcus aureus BAA 41 assessed as inhibition of bacterial growth at 2 ug/ml incubated for 24 hrs by time-kill assay2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1850163Bactericidal activity against methicillin-resistant Staphylococcus aureus BAA 41 assessed as inhibition of bacterial growth at 1 ug/ml incubated for 24 hrs by time-kill assay2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1326329Inhibition of Staphylococcus aureus FtsZ GTPase activity2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Recent advances in the discovery and development of antibacterial agents targeting the cell-division protein FtsZ.
AID394556Bactericidal activity against Staphylococcus aureus ATCC 29213 assessed as reduction in cell viability at 2 ug/ml within 2 hrs by serial dilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1591548Ratio of MBC for penicillin-resistant Staphylococcus aureus clinical isolate to MIC for penicillin-resistant Staphylococcus aureus clinical isolate2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID394553Inhibition of cell division in Bacillus subtilis 168 assessed as elongation of cells at 2 ug/ml by phase contrast microscopy2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1591550Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as log reduction in viable bacterial count at 2 ug/ml incubated for 24 hrs by time-kill curve assay2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1533844Antibacterial activity against Staphylococcus aureus ATCC 29213 by broth microdilution assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Boosting the efficacy of anti-MRSA β-lactam antibiotics via an easily accessible, non-cytotoxic and orally bioavailable FtsZ inhibitor.
AID1850168Ratio of MBC for bactericidal activity against methicillin-resistant Staphylococcus aureus BAA 41 to MIC for antibacterial activity against methicillin-resistant Staphylococcus aureus BAA 412022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1811677Displacement of free fluorescent probe from inter domain cleft of stabilized Bacillus subtilis FtsZ assessed as dissociation constant in presence of GMPCPP by fluorescence anisotropy analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Targeting the FtsZ Allosteric Binding Site with a Novel Fluorescence Polarization Screen, Cytological and Structural Approaches for Antibacterial Discovery.
AID1414191Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID1850143Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as inhibition of bacterial growth incubated for 18 hrs by CLSI protocol based two fold serial dilution method2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1120513Antimicrobial activity against Bacillus subtilis subsp. subtilis str. 168 after 18 hrs by macro-dilution method2013MedChemComm, Jan-01, Volume: 4, Issue:1
Inhibitors of bacterial tubulin target bacterial membranes
AID1677803Antibacterial activity against Escherichia coli ATCC25922 incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID1414216Antibacterial activity against Staphylococcus aureus2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID1811676Antimicrobial activity against methicillin resistant Staphylococcus aureus Mu50 assessed as inhibition of cell division incubated for 1.5 hrs by phase contrast microscopic analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Targeting the FtsZ Allosteric Binding Site with a Novel Fluorescence Polarization Screen, Cytological and Structural Approaches for Antibacterial Discovery.
AID1677807Antibacterial activity against Staphylococcus aureus ATCC25923 incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID1374404Antibacterial activity against Staphylococcus aureus ATCC 25923 after 24 hrs by broth microdilution method2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Substitution of terminal amide with 1H-1,2,3-triazole: Identification of unexpected class of potent antibacterial agents.
AID394531Antibacterial activity against Pseudomonas aeruginosa by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID394534Cytotoxicity against human HepG2 cells2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID394559Inhibition of bovine brain tubulin polymerization at 64 ug/ml2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1850156Antibacterial activity against Bacillus subtilis 168 assessed as cell elongation at 0.5 ug/ml incubated for 4 hrs by phase-contrast microscopy2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1850170Inhibition of Staphylococcus aureus FtsZ polymerization assessed as increase in GTPase activity at 8 ug/ml incubated for 40 mins in presence of GTP by malachite green phosphate assay2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1850165Bactericidal activity against methicillin-resistant Staphylococcus aureus BAA 41 assessed as inhibition of bacterial growth at 4 ug/ml incubated for 24 hrs by time-kill assay2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1850138Antibacterial activity against Bacillus subtilis 168 assessed as inhibition of bacterial growth incubated for 18 hrs by CLSI protocol based two-fold serial dilution assay2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID394527Antibacterial activity against Staphylococcus warneri by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1414188Antibacterial activity against Bacillus subtilis ATCC 9372 after 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID394540Antibacterial activity against Staphylococcus aureus bearing FtsZ G266S mutant by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1850169Inhibition of Staphylococcus aureus FtsZ polymerization assessed as increase in GTPase activity at 1 ug/ml incubated for 40 mins in presence of GTP by malachite green phosphate assay2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1591547Ratio of MBC for methicillin-resistant Staphylococcus aureus ATCC 43300 to MIC for methicillin-resistant Staphylococcus aureus ATCC 433002019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1201479Inhibition of Staphylococcus aureus FtsZ GTPase activity2015European journal of medicinal chemistry, May-05, Volume: 95Advances in the discovery of novel antimicrobials targeting the assembly of bacterial cell division protein FtsZ.
AID394538Antibacterial activity against Staphylococcus aureus bearing FtsZ V214F mutant by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1850144Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as inhibition of bacterial growth incubated for 18 hrs by CLSI protocol based two fold serial dilution method2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1850173Inhibition of Staphylococcus aureus FtsZ polymerization assessed as increase in GTPase activity at 5 to 20 ug/ml incubated for 40 mins in presence of GTP by malachite green phosphate assay2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1374403Antibacterial activity against Bacillus subtilis ATCC 9372 after 24 hrs by broth microdilution method2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Substitution of terminal amide with 1H-1,2,3-triazole: Identification of unexpected class of potent antibacterial agents.
AID1677808Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC43300 incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID1628116Antimicrobial activity against Staphylococcus aureus2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
Targeting the Bacterial Division Protein FtsZ.
AID1374408Antibacterial activity against Klebsiella pneumoniae ATCC 700603 after 24 hrs by broth microdilution method2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Substitution of terminal amide with 1H-1,2,3-triazole: Identification of unexpected class of potent antibacterial agents.
AID394549Antibacterial activity against Staphylococcus aureus Smith ATCC 19636 in iv dosed CD1 mouse septicemia model assessed as survival after 7 days2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1850139Antibacterial activity against Staphylococcus aureus 29213 assessed as inhibition of bacterial growth incubated for 18 hrs by CLSI protocol based two fold serial dilution method2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1534169Inhibition of Staphylococcus aureus N-terminal 6His-tagged FtsZ GTPase expressed in Escherichia coli BL21 (DE3) at 100 uM relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163Boosting the efficacy of anti-MRSA β-lactam antibiotics via an easily accessible, non-cytotoxic and orally bioavailable FtsZ inhibitor.
AID1850142Antibacterial activity against methicillin-resistant Staphylococcus aureus BAA 44 assessed as inhibition of bacterial growth incubated for 18 hrs by CLSI protocol based two fold serial dilution method2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1326328Antibacterial activity against multi-drug resistant Staphylococcus aureus2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Recent advances in the discovery and development of antibacterial agents targeting the cell-division protein FtsZ.
AID394529Antibacterial activity against Escherichia coli by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1591541Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1850140Antibacterial activity against Escherichia coli 25922 assessed as inhibition of bacterial growth incubated for 18 hrs by CLSI protocol based two fold serial dilution method2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1120510Induction of transmembrane potential loss in Bacillus subtilis subsp. subtilis str. 168 at 1 times MIC pre-treated for 5 mins and measured 15 mins post dye addition by DiOC2 dye based flow cytometry2013MedChemComm, Jan-01, Volume: 4, Issue:1
Inhibitors of bacterial tubulin target bacterial membranes
AID1591538Antibacterial activity against Bacillus subtilis ATCC 9372 incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1120509Increase in bacterial membrane permeability in Bacillus subtilis subsp. subtilis str. 168 at 1 times MIC pre-treated for 5 mins and measured 30 mins post dye addition by propidium iodide dye based flow cytometry2013MedChemComm, Jan-01, Volume: 4, Issue:1
Inhibitors of bacterial tubulin target bacterial membranes
AID1533847Bactericidal activity against Staphylococcus aureus ATCC BAA-41 assessed as log reduction in bacterial growth at 2 to 4 times MIC up to 7 hrs by time kill assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Boosting the efficacy of anti-MRSA β-lactam antibiotics via an easily accessible, non-cytotoxic and orally bioavailable FtsZ inhibitor.
AID1591539Antibacterial activity against Bacillus pumilus CMCC63202 incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID394545Bactericidal activity against Staphylococcus aureus ATCC 29213 assessed as logarithmic reduction in viable cell numbers at >= MIC after 24 hrs2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1850145Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33592 assessed as inhibition of bacterial growth incubated for 18 hrs by CLSI protocol based two fold serial dilution method2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID394530Antibacterial activity against Haemophilus influenzae by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID394543Antibacterial activity against Bacillus subtilis bearing FtsZ V307R mutant by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1534181Synergistic bactericidal activity against Staphylococcus aureus ATCC BAA-41 at 1 to 16 times MIC in presence of methicillin up to 24 hrs by time kill assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Boosting the efficacy of anti-MRSA β-lactam antibiotics via an easily accessible, non-cytotoxic and orally bioavailable FtsZ inhibitor.
AID1850147Synergistic antibacterial activity against Escherichia coli 25922 assessed as inhibition of bacterial growth incubated for 18 hrs in presence of PMBN by checkerboard assay2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID394525Antibacterial activity against Staphylococcus lugdunensis by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID394535Antibacterial activity against Staphylococcus aureus bearing FtsZ R191P mutant by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1811670Bactericidal activity against Staphylococcus aureus assessed as reduction in colony forming units2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Targeting the FtsZ Allosteric Binding Site with a Novel Fluorescence Polarization Screen, Cytological and Structural Approaches for Antibacterial Discovery.
AID394541Antibacterial activity against Bacillus subtilis bearing FtsZ A47P mutant by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1591546Ratio of MBC for Staphylococcus aureus ATCC 25923 to MIC for Staphylococcus aureus ATCC 259232019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1591542Antibacterial activity against penicillin-resistant Staphylococcus aureus clinical isolate incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID394552Inhibition of GFP-FtsZ localization in Bacillus subtilis 2020 assessed as protein mislocalization to assemble into cytokinetic ring at 8 ug/ml by florescence microscopy2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1326337Half life in iv dosed BALB/c mouse administered 1 hr after ABT addition by LC-MS/MS analysis2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Recent advances in the discovery and development of antibacterial agents targeting the cell-division protein FtsZ.
AID1120500Induction of membrane associated proteins mislocalization in Bacillus subtilis subsp. subtilis str. 168 assessed as reduction in GFP-MinD protein localization by fluorescence assay2013MedChemComm, Jan-01, Volume: 4, Issue:1
Inhibitors of bacterial tubulin target bacterial membranes
AID1677806Antibacterial activity against Bacillus pumilus CMCC63202 incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID1534167Inhibition of Staphylococcus aureus N-terminal 6His-tagged FtsZ GTPase expressed in Escherichia coli BL21 (DE3) at 30 uM relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163Boosting the efficacy of anti-MRSA β-lactam antibiotics via an easily accessible, non-cytotoxic and orally bioavailable FtsZ inhibitor.
AID1850167Bactericidal activity against methicillin-resistant Staphylococcus aureus BAA 41 assessed as inhibition of bacterial growth incubated for 24 hrs by time-kill assay2022RSC medicinal chemistry, Jan-27, Volume: 13, Issue:1
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism.
AID1533846Selective index, ratio of IC50 for mouse L929 cells to MIC for Staphylococcus aureus ATCC 292132019European journal of medicinal chemistry, Feb-01, Volume: 163Boosting the efficacy of anti-MRSA β-lactam antibiotics via an easily accessible, non-cytotoxic and orally bioavailable FtsZ inhibitor.
AID1374406Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after 24 hrs by broth microdilution method2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Substitution of terminal amide with 1H-1,2,3-triazole: Identification of unexpected class of potent antibacterial agents.
AID394536Antibacterial activity against Staphylococcus aureus bearing FtsZ G193D mutant by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1326330Toxicity in mouse infected with Staphylococcus aureus assessed as survival at 30 mg/kg, iv or po2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Recent advances in the discovery and development of antibacterial agents targeting the cell-division protein FtsZ.
AID394544Antibacterial activity against Bacillus subtilis bearing FtsZ V307H mutant by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID394521Antibacterial activity against multidrug-resistant Staphylococcus aureus by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1060727Antibacterial activity against Staphylococcus aureus harboring FtsZ G196A mutant by broth microdilution method2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Design, synthesis and structure-activity relationships of substituted oxazole-benzamide antibacterial inhibitors of FtsZ.
AID394524Antibacterial activity against Staphylococcus hominis by broth microdilution method2008Science (New York, N.Y.), Sep-19, Volume: 321, Issue:5896
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
AID1414193Antibacterial activity against Escherichia coli ATCC 25922 after 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID1533845Cytotoxicity against mouse L929 cells by MTS assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Boosting the efficacy of anti-MRSA β-lactam antibiotics via an easily accessible, non-cytotoxic and orally bioavailable FtsZ inhibitor.
AID1811675Antimicrobial activity against Bacillus subtilis 168 assessed as inhibition of cell division incubated for 1.5 hrs by phase contrast microscopic analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Targeting the FtsZ Allosteric Binding Site with a Novel Fluorescence Polarization Screen, Cytological and Structural Approaches for Antibacterial Discovery.
AID1374405Antibacterial activity against penicillin-resistant Staphylococcus aureus after 24 hrs by broth microdilution method2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Substitution of terminal amide with 1H-1,2,3-triazole: Identification of unexpected class of potent antibacterial agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (38)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (5.26)29.6817
2010's31 (81.58)24.3611
2020's5 (13.16)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.25

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 Index22.25 (24.57)
Research Supply Index3.66 (2.92)
Research Growth Index5.33 (4.65)
Search Engine Demand Index21.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.25)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (7.89%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other35 (92.11%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]