Page last updated: 2024-11-13
rpx7009
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
RPX7009: a beta-lactamase inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
ID Source | ID |
---|---|
PubMed CID | 56649692 |
CHEMBL ID | 3317857 |
SCHEMBL ID | 620289 |
MeSH ID | M000608394 |
Synonyms (44)
Synonym |
---|
chembl3317857 , |
bdbm50089084 |
IOOWNWLVCOUUEX-WPRPVWTQSA-N |
2-((3r,6s)-2-hydroxy-3-(2-(thiophen-2-yl)acetamido)-1,2-oxaborinan-6-yl)acetic acid |
SCHEMBL620289 |
vaborbactam |
rpx 7009 |
vaborbactam [usan:inn] |
1360457-46-0 |
unii-1c75676f8v |
vaborbactam component of carbavance |
1,2-oxaborinane-6-acetic acid, 2-hydroxy-3-((2-(2-thienyl)acetyl)amino)-, (3r,6s)- |
vaborbactam [usan] |
vabomere component vaborbactam |
rpx-7009 |
vaborbactam [orange book] |
vaborbactam [mi] |
1575712-03-6 |
rpx7009 |
carbavance component vaborbactam |
vaborbactam [who-dd] |
1C75676F8V , |
vaborbactam [inn] |
HY-19930 |
CS-6445 |
D10998 |
vaborbactam (usan/inn) |
DB12107 |
{(3r,6s)-2-hydroxy-3-[(thiophen-2-ylacetyl)amino]-1,2-oxaborinan-6-yl}acetic acid |
AKOS032961376 |
mfcd28502176 |
EX-A2589 |
vaborbactam. rpx7009 |
gtpl10871 |
vabomere (vaborbactam + meropenem) |
NCGC00510003-01 |
compound 9f [pmid: 25782055] |
Q27252228 |
MS-24261 |
2-[(3r,6s)-2-hydroxy-3-[(2-thiophen-2-ylacetyl)amino]oxaborinan-6-yl]acetic acid |
BV163750 |
DTXSID901027690 |
EN300-20818376 |
2-[(3r,6s)-2-hydroxy-3-[2-(thiophen-2-yl)acetamido]-1,2-oxaborinan-6-yl]acetic acid |
Research Excerpts
Overview
RPX7009 is a novel β-lactamase inhibitor with activity against serine carbapenemases.
Excerpt | Reference | Relevance |
---|---|---|
"RPX7009 is a novel β-lactamase inhibitor with activity against serine carbapenemases." | ( Activity of Meropenem Combined with RPX7009, a Novel β-Lactamase Inhibitor, against Gram-Negative Clinical Isolates in New York City. Abdallah, M; Cortes, C; Landman, D; Lapuebla, A; Olafisoye, O; Quale, J; Urban, C, 2015) | 1.41 |
Toxicity
Pharmacokinetics
Excerpt | Reference | Relevance |
---|---|---|
"Vaborbactam (formerly RPX7009) is a member of a new class of β-lactamase inhibitor with pharmacokinetic properties similar to those of many β-lactams, including carbapenems." | ( Phase 1 Study of the Safety, Tolerability, and Pharmacokinetics of the β-Lactamase Inhibitor Vaborbactam (RPX7009) in Healthy Adult Subjects. Dudley, MN; Durso, S; Griffith, DC; Loutit, JS; Morgan, EE, 2016) | 0.96 |
" The pharmacokinetics of meropenem and vaborbactam were similar when given alone or in combination; all evaluated plasma PK exposure measures (peak plasma concentration, area under the plasma concentration-time curve [AUC] from time zero to the last measurable concentration area under the plasma concentration-time curve, and AUC from time zero to infinity) were similar for the study drugs alone versus those in combination, indicating no pharmacokinetic interaction between meropenem and vaborbactam." | ( Phase 1 Study of the Safety, Tolerability, and Pharmacokinetics of Vaborbactam and Meropenem Alone and in Combination following Single and Multiple Doses in Healthy Adult Subjects. Bhavnani, SM; Dudley, MN; Griffith, DC; Loutit, JS; Morgan, EE; Rubino, CM; White, D, 2018) | 0.48 |
" Population pharmacokinetic (PK) models were developed to characterize the time course of meropenem and vaborbactam using pooled data from two phase 1 and two phase 3 studies." | ( Population Pharmacokinetics of Meropenem and Vaborbactam Based on Data from Noninfected Subjects and Infected Patients. Ambrose, PG; Bhavnani, SM; Dudley, MN; Griffith, DC; Loutit, JS; Rubino, CM; Trang, M, 2021) | 0.62 |
Compound-Compound Interactions
Excerpt | Reference | Relevance |
---|---|---|
" It is being developed in combination with meropenem." | ( In vitro activity of meropenem combined with vaborbactam against KPC-producing Enterobacteriaceae in China. Chen, X; Kudinha, T; Lomovskaya, O; Sun, D; Xu, Y; Xu, Z; Yang, Q; Zhang, G; Zhou, M, 2018) | 0.48 |
" In this study, we analyzed the in vitro activity of those novel antibacterial agents alone or in combination with polymyxin B against the CR-A." | ( In vitro activity of ceftazidime/avibactam, imipenem/relebactam and meropenem/vaborbactam alone or in combination with polymyxin B against carbapenem resistant Acinetobacter baumannii. Gu, Y; Hu, D; Hu, M; Liang, R; Wang, D; Wang, M; Zhu, M, 2023) | 0.91 |
Bioavailability
Excerpt | Reference | Relevance |
---|---|---|
" When isolated under acidic conditions, these compounds spontaneously formed a neutral cyclic anhydride (intramolecular prodrug) which was shown to have much-improved oral bioavailability (52-69%) compared to the ring-opened carboxylate salt (9%)." | ( Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability. Clifton, MC; Griffith, DC; Hecker, SJ; Lomovskaya, O; Raja Reddy, K; Tarazi, Z; Totrov, M, 2022) | 0.72 |
Dosage Studied
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (15)
Potency Measurements
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Inhibition Measurements
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Beta-lactamase | Escherichia coli | Ki | 0.0560 | 0.0110 | 0.0335 | 0.0560 | AID1657152 |
Prothrombin | Homo sapiens (human) | IC50 (µMol) | 1,000.0000 | 0.0000 | 0.7107 | 10.0000 | AID1225828 |
Plasminogen | Homo sapiens (human) | IC50 (µMol) | 1,000.0000 | 0.0250 | 3.6280 | 10.0000 | AID1225827 |
Urokinase-type plasminogen activator | Homo sapiens (human) | IC50 (µMol) | 1,000.0000 | 0.0370 | 3.3859 | 10.0000 | AID1225829 |
Tissue-type plasminogen activator | Homo sapiens (human) | IC50 (µMol) | 1,000.0000 | 0.0340 | 2.5425 | 6.6000 | AID1225831 |
Trypsin-1 | Homo sapiens (human) | IC50 (µMol) | 1,000.0000 | 0.0035 | 1.5321 | 10.0000 | AID1225823 |
Trypsin-2 | Homo sapiens (human) | IC50 (µMol) | 1,000.0000 | 0.0035 | 1.5846 | 4.4000 | AID1225823 |
Neutrophil elastase | Homo sapiens (human) | IC50 (µMol) | 1,000.0000 | 0.0063 | 2.0734 | 22.3780 | AID1225834 |
Lysosomal protective protein | Homo sapiens (human) | IC50 (µMol) | 1,000.0000 | 0.6000 | 6.6000 | 10.0000 | AID1225835 |
Chymase | Homo sapiens (human) | IC50 (µMol) | 1,000.0000 | 0.0260 | 2.6397 | 10.0000 | AID1225832 |
Trypsin-3 | Homo sapiens (human) | IC50 (µMol) | 1,000.0000 | 0.0035 | 1.5846 | 4.4000 | AID1225823 |
Beta-lactamase | Acinetobacter baumannii | Ki | 40.0000 | 1.7000 | 1.7000 | 1.7000 | AID1657160 |
Dipeptidyl peptidase 2 | Homo sapiens (human) | IC50 (µMol) | 1,000.0000 | 0.0002 | 0.9316 | 6.6000 | AID1225833 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Biological Processes (109)
Molecular Functions (30)
Ceullar Components (39)
Bioassays (272)
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1225915 | Inhibition of Klebsiella pneumoniae KP1004 TEM-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1588035 | Inhibition of recombinant bacterial L1 expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1559335 | Inhibition of KPC-2/SHV12/TEM-1 in Klebsiella pneumoniae CDC-0361 assessed as cefepime antibacterial activity at 8 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 32 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225780 | Inhibition of Enterobacter cloacae ECL1003 TEM assessed as cefepime MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559327 | Inhibition of KPC-2/SHV12/TEM-1 in Klebsiella pneumoniae CDC-0361 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225857 | Clearance in human at 1 g administered as 3 hrs of infusion | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1832299 | Inhibition of Pseudomonas aeruginosa PBP3 using bocillin FL as a fluorogenic substrate assessed as residual activity at 1 mM preincubated for 1 hr followed by substrate addition measured after 30 mins by fluorescence anisotropy assay relative to control | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15 | High-Throughput Crystallography Reveals Boron-Containing Inhibitors of a Penicillin-Binding Protein with Di- and Tricovalent Binding Modes. |
AID1471284 | Inhibition of bacterial CTX-M by measuring nitrocefin degradation | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 | Pharmaceutical Approaches to Target Antibiotic Resistance Mechanisms. |
AID1588033 | Inhibition of recombinant bacterial VIM-2 expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1864429 | Inhibition of NLRP3 inflammasome activation in LPS-primed mouse J774.A1 cells assessed as reduction in IL-1beta secretion at 1 uM relative to control | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18 | Discovery of a Novel Oral Proteasome Inhibitor to Block NLRP3 Inflammasome Activation with Anti-inflammation Activity. |
AID1225912 | Inhibition of Klebsiella oxytoca KX1017 OXA-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1891032 | Potentiation of aztreonam-induced antibacterial activity against Escherichia coli 1010 producing CMY-6 assessed as concentration required to reduce aztreonam MIC to 4 ug/ml by CLSI based broth microdilution method | 2022 | Bioorganic & medicinal chemistry, 05-15, Volume: 62 | Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability. |
AID1891021 | Potentiation of aztreonam-induced antibacterial activity against Escherichia coli 308 producing SHV-5 assessed as concentration required to reduce aztreonam MIC to 4 ug/ml by CLSI based broth microdilution method | 2022 | Bioorganic & medicinal chemistry, 05-15, Volume: 62 | Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability. |
AID1657154 | Inhibition of recombinant Escherichia coli NDM-1 using imipenem as substrate preincubated for 10 mins followed by substrate addition and measured every 30 secs for 30 mins by spectrophotometric analysis | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 | Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases. |
AID1559329 | Inhibition of KPC-2/PDC-42 in Pseudomonas aeruginosa CDC-0457 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 64 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225764 | Inhibition of Escherichia coli recombinant CMY-2 assessed as substrate nitrocefin degradation preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559308 | Inhibition of bacterial KPC-2 using imipenem as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1695048 | Irreversible inhibition of beta lactamase KPC-2 in Klebsiella pneumoniae assessed as off-rate constant using nitrocefin as substrate preincubated for 30 mins followed by substrate addition | 2020 | RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4 | Cyclic boronates as versatile scaffolds for KPC-2 β-lactamase inhibition. |
AID1225825 | Cmax in rat at 100 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225937 | Inhibition of Klebsiella oxytoca KX1019 KPC-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225753 | Inhibition of Klebsiella pneumoniae KP1088 KPC-3 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225827 | Inhibition of plasmin (unknown origin) using H-D-VLK-pNA as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1471283 | Inhibition of bacterial KPC by measuring nitrocefin degradation | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 | Pharmaceutical Approaches to Target Antibiotic Resistance Mechanisms. |
AID1225747 | Inhibition of Klebsiella pneumoniae KP1008 KPC-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559343 | Inhibition of KPC-2/SHV12/TEM-1 in Klebsiella pneumoniae CDC-0361 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 16 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225758 | Antibacterial activity against Klebsiella pneumoniae KP1004 by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559341 | Inhibition of OXA-232/OXA-9/TEM-1A/CTX-M-15/OXA-1 in Klebsiella pneumoniae CDC-0066 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 32 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225925 | Inhibition of Klebsiella pneumoniae KP1088 TEM-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225891 | Inhibition of Klebsiella pneumoniae KP1088 SHV-11 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225918 | Inhibition of Klebsiella pneumoniae KP1082 KPC-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225812 | Inhibition of Enterobacter cloacae ECL1058 TEM-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225907 | Inhibition of Enterobacter cloacae ECL1058 SHV-11 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225928 | Inhibition of Klebsiella pneumoniae KP1084 TEM-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1471285 | Inhibition of bacterial SHV by measuring nitrocefin degradation | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 | Pharmaceutical Approaches to Target Antibiotic Resistance Mechanisms. |
AID1225833 | Inhibition of dipeptidyl peptidase 7 (unknown origin) using H-Lys-Pro-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1525845 | Inhibition of bacterial class B1 metallo beta-lactamase NDM-1 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases. |
AID1525846 | Inhibition of bacterial class B1 metallo beta-lactamase VIM-1 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases. |
AID1225820 | Inhibition of Klebsiella pneumoniae KP1084 TEM-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225892 | Inhibition of Klebsiella pneumoniae KP1088 TEM-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225848 | Clearance in rat at 1000 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225870 | Inhibition of Enterobacter cloacae EC1010 CMY-6 assessed as cefepime MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225824 | Inhibition of chymotrypsin (unknown origin) using Suc-AAPF-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225943 | Inhibition of Klebsiella pneumoniae KP1004 TEM-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225809 | Inhibition of Klebsiella oxytoca KX1017 OXA-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225858 | Volume of distribution at steady state in human at 1 g administered as 3 hrs of infusion | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225894 | Inhibition of Klebsiella pneumoniae KP1083 TEM-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1695046 | Inhibition of beta lactamase KPC-2 in Klebsiella pneumoniae assessed as apparent inhibition constant using nitrocefin as substrate measured without preincubation by Dixon plot analysis | 2020 | RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4 | Cyclic boronates as versatile scaffolds for KPC-2 β-lactamase inhibition. |
AID1225830 | Inhibition of elastase (unknown origin) using Suc-AAPA-pNA as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1525843 | Inhibition of bacterial class A serine beta-lactamase TEM-116 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases. |
AID1588027 | Inhibition of Escherichia coli TEM-116 assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1225823 | Inhibition of trypsin (unknown origin) using N-Bz-R-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225883 | Inhibition of Klebsiella pneumoniae KP1004 SHV-11 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1588044 | Inhibition of NDM1 in Klebsiella pneumoniae B64 clinical isolate assessed as potentiation of meropenem-induced antibacterial activity by measuring meropenem MIC at 8 ug/ml by broth microdilution method (Rvb > 64 ug/ml) | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1225846 | Half life in rat at 1000 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559323 | Inhibition of VIM-27/CTX-M-15/SHV-11/OXA-1 in Klebsiella pneumoniae CDC-0040 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225813 | Inhibition of Enterobacter cloacae ECL1058 SHV-11 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225899 | Inhibition of Klebsiella pneumoniae KP1084 SHV-11 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1588029 | Inhibition of recombinant bacterial KPC-2 expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1225835 | Inhibition of cathepsin A (unknown origin) using MCA-RPPGFSAFK-Dnp as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1529342 | Inhibition of beta lactamase KPC in Enterobacteriaceae assessed as potentiation of meropenem-induced antibacterial activity by measuring meropenem MIC by broth microdilution method | 2018 | MedChemComm, Sep-01, Volume: 9, Issue:9 | β-lactam/β-lactamase inhibitor combinations: an update. |
AID1225933 | Inhibition of Escherichia coli EC1007 KPC-3 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225941 | Inhibition of Klebsiella oxytoca KX1017 SHV-30 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1588042 | Inhibition of NDM1 in Escherichia coli S117 clinical isolate assessed as potentiation of meropenem-induced antibacterial activity by measuring meropenem MIC at 8 ug/ml by broth microdilution method (Rvb > 64 ug/ml) | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1225923 | Inhibition of Klebsiella pneumoniae KP1088 KPC-3 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1183472 | Inhibition of beta-lactamase (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16 | Confronting the challenges of discovery of novel antibacterial agents. |
AID1225917 | Inhibition of Klebsiella pneumoniae KP1008 KPC-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1588034 | Inhibition of recombinant bacterial CphA expressed in Escherichia coli assessed as reduction in hydrolysis of meropenem by UV spectrophotometeric analysis | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1525848 | Inhibition of Aeromonas hydrophila class B2 metallo beta-lactamse CphA assessed as reduction in meropenem hydrolysis after 10 mins by UV absorbance method | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases. |
AID1225800 | Inhibition of Klebsiella pneumoniae KP1083 KPC-3 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225888 | Inhibition of Klebsiella pneumoniae KP1083 SHV-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1588043 | Inhibition of NDM1 in Escherichia coli IR57 clinical isolate assessed as potentiation of meropenem-induced antibacterial activity by measuring meropenem MIC at 8 ug/ml by broth microdilution method (Rvb > 64 ug/ml) | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1559320 | Inhibition of bacterial NDM-1 using cefepime as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225930 | Inhibition of Klebsiella pneumoniae KP1087 CTX-M-15 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225804 | Inhibition of Klebsiella pneumoniae KP1004 SHV-11 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225808 | Inhibition of Klebsiella oxytoca KX1017 KPC-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225901 | Inhibition of Klebsiella pneumoniae KP1087 KPC-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1525854 | Inhibition of bacterial class D serine beta-lactamase OXA-48 assessed as reduction in breakdown of cephalosporin FC-5 in presence of aqueous sodium bicarbonate after 10 mins by fluorescence method | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases. |
AID1225863 | Inhibition of Klebsiella pneumoniae KP1005 CTX-M-14 assessed as cefepime MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225748 | Inhibition of Klebsiella pneumoniae KP1082 KPC-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225851 | In vivo inhibition of KPC in Klebsiella pneumoniae KP1074 in Swiss webster neutropenic mouse lung infection model assessed as biapenem deltalog10CFU in lung at 50 mg/kg, ip administered every 2 hrs starting at 2 hrs postinfection measured after 24 hrs | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225836 | Half life in rat at 100 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225898 | Inhibition of Klebsiella pneumoniae KP1084 KPC-3 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225842 | Volume of distribution in rat at 300 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225900 | Inhibition of Klebsiella pneumoniae KP1084 TEM-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1529341 | Inhibition of beta lactamase KPC in Klebsiella pneumoniae BAA-1705 assessed as potentiation of meropenem-induced antibacterial activity by measuring fold reduction in meropenem MIC90 by checkerboard microdilution assay relative to meropenem alone | 2018 | MedChemComm, Sep-01, Volume: 9, Issue:9 | β-lactam/β-lactamase inhibitor combinations: an update. |
AID1225822 | Inhibition of Klebsiella pneumoniae KP1084 SHV-11 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225940 | Inhibition of Klebsiella oxytoca KX1017 OXA-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1471286 | Inhibition of bacterial CMY by measuring nitrocefin degradation | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 | Pharmaceutical Approaches to Target Antibiotic Resistance Mechanisms. |
AID1225871 | Inhibition of Klebsiella oxytoca KX1001 OXA-2 assessed as cefepime MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225862 | Inhibition of Escherichia coli EC1008 CTX-M-3 assessed as cefepime MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225803 | Inhibition of Klebsiella pneumoniae KP1008 KPC-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225868 | Inhibition of Enterobacter cloacae ECL1061 AmpC assessed as cefepime MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1657157 | Inhibition of recombinant Escherichia coli SHV-12 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 | Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases. |
AID1225840 | AUC (0 to infinity) in rat at 300 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1695050 | Potentiation of cefepime-induced antibacterial activity against Klebsiella pneumoniae Ecl8 transfected with pUBYT vector expressing KPC-2 assessed as cefepime MIC measured after 18 to 24 hrs by CLSI protocol based broth microdilution assay (Rvb >=256 ug/m | 2020 | RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4 | Cyclic boronates as versatile scaffolds for KPC-2 β-lactamase inhibition. |
AID1225872 | Inhibition of Enterobacter aerogenes EA1028 OXA-30 assessed as cefepime MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1695047 | Inhibition of beta lactamase KPC-2 in Klebsiella pneumoniae assessed as apparent second order rate constant K2/K using nitrocefin as substrate | 2020 | RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4 | Cyclic boronates as versatile scaffolds for KPC-2 β-lactamase inhibition. |
AID1225875 | Inhibition of Enterobacter cloacae ECL1058 TEM-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225854 | Cmax in human at 1 g administered as 3 hrs of infusion | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225935 | Inhibition of Enterobacter cloacae ECL1058 SHV-11 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225893 | Inhibition of Klebsiella pneumoniae KP1083 SHV-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1529340 | Inhibition of beta lactamase KPC in Klebsiella pneumoniae BAA-1705 assessed as potentiation of meropenem-induced antibacterial activity by measuring fold reduction in meropenem MIC50 by checkerboard microdilution assay relative to meropenem alone | 2018 | MedChemComm, Sep-01, Volume: 9, Issue:9 | β-lactam/β-lactamase inhibitor combinations: an update. |
AID1225884 | Inhibition of Klebsiella pneumoniae KP1008 KPC-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225887 | Inhibition of Klebsiella pneumoniae KP1083 KPC-3 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1588047 | Inhibition of NDM1 in Escherichia coli 91N clinical isolate assessed as potentiation of meropenem-induced antibacterial activity by measuring meropenem MIC at 8 ug/ml by broth microdilution method (Rvb > 64 ug/ml) | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1559345 | Inhibition of KPC-2/PDC-42 in Pseudomonas aeruginosa CDC-0457 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 128 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1657155 | Inhibition of recombinant Escherichia coli CTX-M-14 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 | Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases. |
AID1225914 | Inhibition of Klebsiella pneumoniae KP1004 KPC-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1657156 | Inhibition of recombinant Escherichia coli TEM-10 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 | Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases. |
AID1225942 | Inhibition of Klebsiella pneumoniae KP1004 KPC-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225903 | Inhibition of Klebsiella pneumoniae KP1087 SHV-11 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559317 | Inhibition of bacterial CTX-M-15 using cefotaxime as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1559342 | Inhibition of KPC-2/PDC-42 in Pseudomonas aeruginosa CDC-0356 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 32 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225845 | AUC (0 to infinity) in rat at 1000 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225880 | Inhibition of Klebsiella oxytoca KX1017 SHV-30 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1891030 | Potentiation of aztreonam-induced antibacterial activity against Klebsiella pneumoniae 1004 producing KPC assessed as concentration required to reduce aztreonam MIC to 4 ug/ml by CLSI based broth microdilution method | 2022 | Bioorganic & medicinal chemistry, 05-15, Volume: 62 | Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability. |
AID1225761 | Inhibition of Escherichia coli recombinant SHV-12 assessed as substrate nitrocefin degradation preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225882 | Inhibition of Klebsiella pneumoniae KP1004 TEM-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1657161 | Inhibition of recombinant Escherichia coli VIM-1 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 | Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases. |
AID1225779 | Inhibition of Escherichia coli EC1011 TEM-26 assessed as cefepime MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225843 | Clearance in rat at 300 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225806 | Inhibition of Klebsiella pneumoniae KP1004 KPC-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559337 | Inhibition of KPC-2/PDC-42 in Pseudomonas aeruginosa CDC-0457 assessed as cefepime antibacterial activity at 8 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 16 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1525844 | Inhibition of bacterial class B1 metallo beta-lactamase IMP-1 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases. |
AID1225817 | Inhibition of Klebsiella pneumoniae KP1087 SHV-11 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225756 | In vivo inhibition of KPC in Klebsiella pneumoniae KP1074 in Swiss webster neutropenic mouse lung infection model assessed as meropenem deltalog10CFU in lung at 50 mg/kg, ip administered every 2 hrs starting at 2 hrs postinfection measured after 24 hrs | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1588031 | Inhibition of recombinant bacterial NDM-1 expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1588038 | Inhibition of recombinant Escherichia coli OXA-10 assessed as reduction in breakdown of cephalosporin FC-5 in presence of 100 mM NaHCO3 by fluorescence method | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1225876 | Inhibition of Klebsiella oxytoca KX1019 KPC-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225926 | Inhibition of Klebsiella pneumoniae KP1084 KPC-3 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225909 | Inhibition of Klebsiella oxytoca KX1019 KPC-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559309 | Inhibition of bacterial AmpC using nitrocefin as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1559316 | Inhibition of bacterial SHV-5 using cefotaxime as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225896 | Inhibition of Klebsiella pneumoniae KP1088 SHV-11 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1695045 | Inhibition of beta lactamase KPC-2 in Klebsiella pneumoniae using nitrocefin as substrate preincubated for 10 mins followed by substrate addition | 2020 | RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4 | Cyclic boronates as versatile scaffolds for KPC-2 β-lactamase inhibition. |
AID1225905 | Inhibition of Escherichia coli EC1007 KPC-3 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225844 | Cmax in rat at 1000 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225819 | Inhibition of Klebsiella pneumoniae KP1087 KPC-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1891031 | Potentiation of aztreonam-induced antibacterial activity against Enterobacter cloacae 1002 producing AmpC assessed as concentration required to reduce aztreonam MIC to 4 ug/ml by CLSI based broth microdilution method | 2022 | Bioorganic & medicinal chemistry, 05-15, Volume: 62 | Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability. |
AID1225749 | Inhibition of Klebsiella pneumoniae KP1082 SHV-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225754 | Inhibition of Klebsiella pneumoniae KP1088 SHV-11 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225796 | Inhibition of Klebsiella pneumoniae KP1087 CTX-M-15 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1695049 | Inhibition of beta lactamase KPC-2 in Klebsiella pneumoniae assessed as irreversible covalent complex formation by measuring half life using nitrocefin as substrate | 2020 | RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4 | Cyclic boronates as versatile scaffolds for KPC-2 β-lactamase inhibition. |
AID1588030 | Inhibition of recombinant bacterial IMP-1 expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1559339 | Inhibition of VIM-27/CTX-M-15/SHV-11/OXA-1 in Klebsiella pneumoniae CDC-0040 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225807 | Inhibition of Klebsiella oxytoca KX1017 SHV-30 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1695051 | Potentiation of meropenem-induced antibacterial activity against Klebsiella pneumoniae Ecl8 transfected with pUBYT vector expressing KPC-2 assessed as meropenem MIC measured after 18 to 24 hrs by CLSI protocol based broth microdilution assay (Rvb = 16 ug/ | 2020 | RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4 | Cyclic boronates as versatile scaffolds for KPC-2 β-lactamase inhibition. |
AID1225798 | Inhibition of Klebsiella pneumoniae KP1087 TEM-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225861 | Inhibition of Enterobacter cloacae ECL1003 SHV assessed as cefepime MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1588037 | Inhibition of recombinant bacterial OXA-10 expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1225794 | Inhibition of Klebsiella pneumoniae KP1084 TEM-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225834 | Inhibition of neutrophil elastase (unknown origin) using MeOSuc-AAVP-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225810 | Inhibition of Klebsiella oxytoca KX1019 OXA-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1657158 | Inhibition of recombinant Escherichia coli AmpC using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 | Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases. |
AID1525849 | Inhibition of Stenotrophomonas maltophilia class B3 metallo beta-lactamse L1 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases. |
AID1225847 | Volume of distribution in rat at 1000 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1657160 | Inhibition of Acinetobacter baumannii OXA-23 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 | Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases. |
AID1559319 | Inhibition of bacterial OXA-1 using nitrocefin as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225760 | Inhibition of Escherichia coli recombinant CTX-M-15 assessed as substrate nitrocefin degradation preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225913 | Inhibition of Klebsiella oxytoca KX1017 SHV-30 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225866 | Inhibition of Klebsiella pneumoniae KP1010 SHV-12 assessed as cefepime MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225885 | Inhibition of Klebsiella pneumoniae KP1082 KPC-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225752 | Inhibition of Klebsiella pneumoniae KP1083 TEM-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225757 | Inhibition of Klebsiella pneumoniae KP1004 KPC 2 carbapenemase assessed as minimum concentration required to reduce biapenem MIC from 32 ug/ml to 1 ug/mL by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559333 | Inhibition of OXA-232/OXA-9/TEM-1A/CTX-M-15/OXA-1 in Klebsiella pneumoniae CDC-0066 assessed as cefepime antibacterial activity at 8 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1588032 | Inhibition of recombinant bacterial VIM-1 expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1225904 | Inhibition of Klebsiella pneumoniae KP1087 TEM-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225816 | Inhibition of Klebsiella pneumoniae KP1087 TEM-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225877 | Inhibition of Klebsiella oxytoca KX1019 OXA-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559336 | Inhibition of NDM in Escherichia coli CDC-0452 assessed as cefepime antibacterial activity after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 64 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225879 | Inhibition of Klebsiella oxytoca KX1017 OXA-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225890 | Inhibition of Klebsiella pneumoniae KP1088 KPC-3 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225908 | Inhibition of Enterobacter cloacae ECL1058 TEM-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559325 | Inhibition of OXA-232/OXA-9/TEM-1A/CTX-M-15/OXA-1 in Klebsiella pneumoniae CDC-0066 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1832314 | Inhibition of Pseudomonas aeruginosa PBP3 using bocillin FL as a fluorogenic substrate assessed as inhibition constant at 1 to 1024 uM preincubated for 1 hr followed by substrate addition measured after 30 mins by fluorescence anisotropy assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15 | High-Throughput Crystallography Reveals Boron-Containing Inhibitors of a Penicillin-Binding Protein with Di- and Tricovalent Binding Modes. |
AID1225792 | Inhibition of Klebsiella pneumoniae KP1084 KPC-3 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1588045 | Inhibition of NDM1 in Klebsiella pneumoniae B68-1 clinical isolate assessed as potentiation of meropenem-induced antibacterial activity by measuring meropenem MIC at 8 ug/ml by broth microdilution method (Rvb > 64 ug/ml) | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1525850 | Inhibition of Pseudomonas aeruginosa class C serine beta-lactamase AmpC assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases. |
AID1225799 | Inhibition of Escherichia coli EC1007 KPC-3 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559321 | Inhibition of bacterial IMP-1 using nitrocefin as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225881 | Inhibition of Klebsiella pneumoniae KP1004 KPC-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225821 | Inhibition of Klebsiella pneumoniae KP1084 KPC-3 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225916 | Inhibition of Klebsiella pneumoniae KP1004 SHV-11 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225763 | Inhibition of Escherichia coli recombinant P99 assessed as substrate nitrocefin degradation preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225829 | Inhibition of urokinase (unknown origin) using NGK-pNA as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559338 | Inhibition of KPC-2 in Klebsiella pneumoniae ATCC BAA 1705 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 16 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225755 | Inhibition of Klebsiella pneumoniae KP1088 TEM-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225931 | Inhibition of Klebsiella pneumoniae KP1087 SHV-11 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1588036 | Inhibition of recombinant bacterial AmpC expressed in Escherichia coli assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1225828 | Inhibition of thrombin (unknown origin) using Benz-FVR-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225865 | Inhibition of Klebsiella pneumoniae KP1011 SHV5 assessed as cefepime MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1588041 | Inhibition of bacterial expressed in Escherichia coli OXA-10 assessed as reduction in breakdown of cephalosporin FC-5 at 400 uM by fluorescence method | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1559330 | Inhibition of KPC-2 in Klebsiella pneumoniae ATCC BAA 1705 assessed as cefepime antibacterial activity at 8 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 16 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1525847 | Inhibition of bacterial class B1 metallo beta-lactamse VIM-2 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases. |
AID1225906 | Inhibition of Enterobacter cloacae ECL1058 KPC-3 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225938 | Inhibition of Klebsiella oxytoca KX1019 OXA-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225814 | Inhibition of Enterobacter cloacae ECL1058 KPC-3 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225751 | Inhibition of Klebsiella pneumoniae KP1083 SHV-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225811 | Inhibition of Klebsiella oxytoca KX1019 KPC-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225895 | Inhibition of Klebsiella pneumoniae KP1088 KPC-3 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225852 | Toxicity in Swiss webster neutropenic mouse lung infection model up to 1000 mg/kg, administered every 2 hrs starting at 2 hrs | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225927 | Inhibition of Klebsiella pneumoniae KP1084 SHV-11 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225853 | Toxicity in human at 250 to 1500 mg administered as 3 hrs of infusion | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1657152 | Inhibition of recombinant Escherichia coli KPC-2 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition and measured every 10 secs for 10 mins by spectrophotometric analysis | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 | Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases. |
AID1559332 | Inhibition of NDM-1/CMY-6/OXA-1 in Escherichia coli CDC-0055 assessed as cefepime antibacterial activity at 8 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 128 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225795 | Inhibition of Klebsiella pneumoniae KP1087 KPC-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225746 | Inhibition of Klebsiella pneumoniae KP1004 SHV-11 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1891047 | Oral bioavailability in rat | 2022 | Bioorganic & medicinal chemistry, 05-15, Volume: 62 | Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability. |
AID1657162 | Inhibition of recombinant Escherichia coli IMP-1 using imipenem as substrate preincubated for 10 mins followed by substrate addition measured every 30 secs for 30 mins by spectrophotometrically analysis | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 | Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases. |
AID1225805 | Inhibition of Klebsiella pneumoniae KP1004 TEM-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225801 | Inhibition of Klebsiella pneumoniae KP1082 SHV-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559340 | Inhibition of NDM-1/CMY-6/OXA-1 in Escherichia coli CDC-0055 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 32 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225939 | Inhibition of Klebsiella oxytoca KX1017 KPC-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1891028 | Potentiation of aztreonam-induced antibacterial activity against Klebsiella pneumoniae 1009 producing class A CTX-M-14 assessed as concentration required to reduce aztreonam MIC to 4 ug/ml by CLSI based broth microdilution method | 2022 | Bioorganic & medicinal chemistry, 05-15, Volume: 62 | Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability. |
AID1225855 | Half life in human at 1 g administered as 3 hrs of infusion | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1657159 | Inhibition of Acinetobacter baumannii OXA-48 using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometrically analysis | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 | Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases. |
AID1225869 | Inhibition of Enterobacter cloacae ECL1061 KPC-3 assessed as cefepime MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225897 | Inhibition of Klebsiella pneumoniae KP1088 TEM-1 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225924 | Inhibition of Klebsiella pneumoniae KP1088 SHV-11 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225815 | Inhibition of Escherichia coli EC1007 KPC-3 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225874 | Inhibition of Enterobacter cloacae ECL1058 SHV-11 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559326 | Inhibition of KPC-2/PDC-42 in Pseudomonas aeruginosa CDC-0356 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1832301 | Inhibition of Pseudomonas aeruginosa PBP3 using (2-((benzoyl-D-alanyl)thio)acetic acid) as a substrate assessed as residual activity by measuring substrate turnover at 1 mM incubated for 1 hr followed by substrate addition by absorbance based assay relati | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15 | High-Throughput Crystallography Reveals Boron-Containing Inhibitors of a Penicillin-Binding Protein with Di- and Tricovalent Binding Modes. |
AID1225919 | Inhibition of Klebsiella pneumoniae KP1082 SHV-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225902 | Inhibition of Klebsiella pneumoniae KP1087 CTX-M-15 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225826 | AUC (0 to infinity) in rat at 100 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559331 | Inhibition of VIM-27/CTX-M-15/SHV-11/OXA-1 in Klebsiella pneumoniae CDC-0040 assessed as cefepime antibacterial activity at 8 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1559344 | Inhibition of NDM in Escherichia coli CDC-0452 assessed as meropenem antibacterial activity at 4 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb = 32 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225818 | Inhibition of Klebsiella pneumoniae KP1087 CTX-M-15 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225832 | Inhibition of chymase (unknown origin) using Suc-AAPF-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225841 | Half life in rat at 300 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225922 | Inhibition of Klebsiella pneumoniae KP1083 TEM-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559322 | Inhibition of KPC-2 in Klebsiella pneumoniae ATCC BAA 1705 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225762 | Inhibition of Escherichia coli recombinant TEM-10 assessed as substrate nitrocefin degradation preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559328 | Inhibition of NDM in Escherichia coli CDC-0452 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1588039 | Inhibition of recombinant Escherichia coli OXA-48 assessed as reduction in breakdown of cephalosporin FC-5 by fluorescence method | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1225797 | Inhibition of Klebsiella pneumoniae KP1087 SHV-11 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225936 | Inhibition of Enterobacter cloacae ECL1058 TEM-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225837 | Volume of distribution in rat at 100 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1588046 | Inhibition of NDM1 in Klebsiella pneumoniae IR43 clinical isolate assessed as potentiation of meropenem-induced antibacterial activity by measuring meropenem MIC at 8 ug/ml by broth microdilution method (Rvb > 64 ug/ml) | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1225838 | Clearance in rat at 100 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225889 | Inhibition of Klebsiella pneumoniae KP1083 TEM-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225934 | Inhibition of Enterobacter cloacae ECL1058 KPC-3 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559311 | Inhibition of bacterial VIM-2 using nitrocefin as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225778 | Inhibition of Escherichia coli EC1009 TEM-10 assessed as cefepime MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225929 | Inhibition of Klebsiella pneumoniae KP1087 KPC-2 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225856 | AUC in human at 1 g administered as 3 hrs of infusion | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1525851 | Inhibition of bacterial class D serine beta-lactamase OXA-10 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases. |
AID1225759 | Inhibition of Escherichia coli recombinant KPC-2 assessed as substrate nitrocefin degradation preincubated for 10 mins followed by substrate addition measured every 10 secs for 10 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225910 | Inhibition of Klebsiella oxytoca KX1019 OXA-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225839 | Cmax in rat at 300 mg/kg, iv administered as 0.5 hrs infusion by HPLC-MS method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225921 | Inhibition of Klebsiella pneumoniae KP1083 SHV-1 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225878 | Inhibition of Klebsiella oxytoca KX1017 KPC-2 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559324 | Inhibition of NDM-1/CMY-6/OXA-1 in Escherichia coli CDC-0055 assessed as piperacillin antibacterial activity at 16 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1891029 | Potentiation of aztreonam-induced antibacterial activity against Escherichia coli 302 producing TEM-10 assessed as concentration required to reduce aztreonam MIC to 4 ug/ml by CLSI based broth microdilution method | 2022 | Bioorganic & medicinal chemistry, 05-15, Volume: 62 | Broad-spectrum cyclic boronate β-lactamase inhibitors featuring an intramolecular prodrug for oral bioavailability. |
AID1588040 | Inhibition of recombinant Escherichia coli OXA-48 assessed as reduction in breakdown of cephalosporin FC-5 in presence of 100 mM NaHCO3 by fluorescence method | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Profiling interactions of vaborbactam with metallo-β-lactamases. |
AID1559310 | Inhibition of bacterial OXA-48 using nitrocefin as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225802 | Inhibition of Klebsiella pneumoniae KP1082 KPC-2 assessed as meropenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225873 | Inhibition of Enterobacter cloacae ECL1058 KPC-3 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225886 | Inhibition of Klebsiella pneumoniae KP1082 SHV-1 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1525852 | Inhibition of bacterial class D serine beta-lactamase OXA-10 assessed as reduction in breakdown of cephalosporin FC-5 in presence of aqueous sodium bicarbonate after 10 mins by fluorescence method | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases. |
AID1559318 | Inhibition of bacterial CMY-2 using nitrocefin as substrate preincubated for 15 mins followed by susbtrate addition and measured after 10 mins by spectrophotometric method | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1225793 | Inhibition of Klebsiella pneumoniae KP1084 SHV-11 assessed as biapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225867 | Inhibition of Enterobacter cloacae ECL1002 AmpC assessed as cefepime MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225750 | Inhibition of Klebsiella pneumoniae KP1083 KPC-3 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225932 | Inhibition of Klebsiella pneumoniae KP1087 TEM-1 assessed as imipenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225831 | Inhibition of tissue plasminogen activator (unknown origin) using GK-pNA as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225920 | Inhibition of Klebsiella pneumoniae KP1083 KPC-3 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1225864 | Inhibition of Klebsiella pneumoniae KP1009 CTX-M-15 assessed as cefepime MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
AID1559334 | Inhibition of KPC-2/PDC-42 in Pseudomonas aeruginosa CDC-0356 assessed as cefepime antibacterial activity at 8 ug/ml after 16 to 20 hrs by CLSI-based microbroth dilution method (Rvb > 128 ug/ml) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. |
AID1525853 | Inhibition of bacterial class D serine beta-lactamase OXA-48 assessed as reduction in breakdown of cephalosporin FC-5 after 10 mins by fluorescence method | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases. |
AID1225911 | Inhibition of Klebsiella oxytoca KX1017 KPC-2 assessed as ertapenem MIC at 4 ug/ml by broth microdilution method | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (99)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 36 (36.36) | 24.3611 |
2020's | 63 (63.64) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 17.76
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (17.76) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 4 (4.00%) | 5.53% |
Reviews | 14 (14.00%) | 6.00% |
Case Studies | 3 (3.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 79 (79.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |