Compounds > gsk1322322
Page last updated: 2024-11-13

gsk1322322

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Description

GSK1322322: inhibits peptide deformylase; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID52918384
CHEMBL ID3301608
SCHEMBL ID1189985
MeSH IDM0588391

Synonyms (36)

Synonym
gsk-1322322
gsk-322
unii-12m6kfd07e
gsk 1322322
gsk1322322
cyclopentanepropanoic acid, alpha-((formylhydroxyamino)methyl)-, 2-(5-fluoro-6-((9as)-hexahydropyrazino(2,1-c)(1,4)oxazin-8(1h)-yl)-2-methyl-4-pyrimidinyl)hydrazide, (alphar)-
lanopepden [usan:inn]
lanopepden
1152107-25-9
12m6kfd07e ,
lanopepden [who-dd]
gsk-1322322b
lanopepden [inn]
cyclopentanepropanoic acid, .alpha.-((formylhydroxyamino)methyl)-, 2-(5-fluoro-6-((9as)-hexahydropyrazino(2,1-c)(1,4)oxazin-8(1h)-yl)-2-methyl-4-pyrimidinyl)hydrazide, (.alpha.r)-
lanopepden [usan]
gsk1322322b
n-((r)-2-(cyclopentylmethyl)-3-(2-(5-fluoro-6-((s)-hexahydropyrazino[2,1-c][1,4]oxazin-8(1h)-yl)-2-methylpyrimidin-4-yl)hydrazinyl)-3-oxopropyl)-n-hydroxyformamide
CHEMBL3301608
SCHEMBL1189985
[(2r)-2-(cyclopentyl methyl)-3-(2-{5-fluoro-6-[(9as)-hexahydropyrazino[2,1-c][1,4]oxazin-8(1h)-yl]-2-methyl-4-pyrimidinyl}hydrazino)-3-oxopropyl]hydroxyformamide
SWHNZGMQMGFQGW-MSOLQXFVSA-N
[(2r)-2-(cyclopentylmethyl)-3-(2-{5-fluoro-6-[(9as)-hexahydropyrazino[2,1-c][1,4]oxazin-8(1h)-yl]-2-methyl-4-pyrimidinyl}hydrazino)-3-oxopropyl]hydroxyformamide
D10712
lanopepden (usan/inn)
DTXSID00151006
AKOS027321270
cyclopentanepropanoic acid, a-[(formylhydroxyamino)methyl]-, 2-[5-fluoro-6-[(9as)-hexahydropyrazino[2,1-c][1,4]oxazin-8(1h)-yl]-2-methyl-4-pyrimidinyl]hydrazide, (ar)-
DB11912
NB4 ,
n-[(2r)-2-(cyclopentylmethyl)-3-(2-{5-fluoro- 6-[(9as)-hexahydropyrazino[2,1-c][1,4]oxazin-8(1h)-yl]- 2-methylpyrimidin-4-yl}hydrazin-1-yl)-3-oxopropyl]- n-hydroxyformamide
1152107-25-9 (free base)
HY-12480
CS-0011738
Q27251425
n-[(2r)-3-[2-[6-[(9as)-3,4,6,7,9,9a-hexahydro-1h-pyrazino[2,1-c][1,4]oxazin-8-yl]-5-fluoro-2-methylpyrimidin-4-yl]hydrazinyl]-2-(cyclopentylmethyl)-3-oxopropyl]-n-hydroxyformamide
bdbm50535502

Research Excerpts

Overview

GSK1322322 is a novel peptide deformylase (PDF) inhibitor being developed for the intravenous and oral treatment of acute bacterial skin and skin structure infections and hospitalized patients with community-acquired pneumonia. GSK 1322322 has known antibacterial activities against multidrug-resistant respiratory and skin pathogens.

ExcerptReferenceRelevance
"GSK1322322 is a potent inhibitor of peptide deformylase, an essential bacterial enzyme required for protein maturation. "( Single-dose safety, tolerability, and pharmacokinetics of the antibiotic GSK1322322, a novel peptide deformylase inhibitor.
Dumont, E; Jones, LS; Kurtinecz, M; Naderer, OJ; Zhu, J, 2013)		2.06
"GSK1322322 is a novel peptide deformylase (PDF) inhibitor being developed for the intravenous and oral treatment of acute bacterial skin and skin structure infections and hospitalized patients with community-acquired pneumonia. "( Comparative analysis of the antibacterial activity of a novel peptide deformylase inhibitor, GSK1322322.
Aubart, K; Bouchillon, S; Butler, D; Hackel, M; Hightower, S; Hoban, D; O'Dwyer, K; Qin, D; Zalacain, M, 2013)		2.05
"GSK1322322 is a potent inhibitor of peptide deformylase, an essential bacterial enzyme required for protein maturation. "( Safety, tolerability and pharmacokinetics of repeat dosing of the antibiotic GSK1322322, a peptide deformylase inhibitor: a randomized placebo-controlled study.
Dumont, E; Jones, LS; Kurtinecz, M; Naderer, OJ; Zhu, J, 2013)		2.06
"GSK1322322 is a novel PDF inhibitor that is in phase II clinical development for the treatment of lower respiratory tract and skin infections."( Potent sub-MIC effect of GSK1322322 and other peptide deformylase inhibitors on in vitro growth of Staphylococcus aureus.
Aubart, K; Butler, D; Chen, D; Lewandowski, T; O'Dwyer, K; Zalacain, M, 2014)		1.43
"GSK1322322 is a potent peptide deformylase inhibitor with in vitro and in vivo activity against multidrug-resistant skin and respiratory pathogens. "( Penetration of GSK1322322 into epithelial lining fluid and alveolar macrophages as determined by bronchoalveolar lavage.
Bowen, CL; Chen, L; Dumont, E; Jones, LS; Naderer, OJ; Rodvold, KA; Zhu, JZ, 2014)		2.2
"GSK1322322 is a novel antibacterial agent under development, and it has known antibacterial activities against multidrug-resistant respiratory and skin pathogens through its inhibition of the bacterial peptide deformylase. "( Microbiome changes in healthy volunteers treated with GSK1322322, a novel antibiotic targeting bacterial peptide deformylase.
Arat, S; Aubart, K; Brown, JR; Holmes, DJ; Ingraham, K; Jones, L; Livi, GP; Naderer, O; Sathe, G; Spivak, A; Thomas, E; Traini, C; Van Horn, S, 2015)		2.11
"GSK1322322 is a peptide deformylase inhibitor active against Staphylococcus aureus strains resistant to currently marketed antibiotics. "( Cellular pharmacokinetics and intracellular activity of the novel peptide deformylase inhibitor GSK1322322 against Staphylococcus aureus laboratory and clinical strains with various resistance phenotypes: studies with human THP-1 monocytes and J774 murine
Butler, D; Peyrusson, F; Tulkens, PM; Van Bambeke, F, 2015)		2.08
"GSK1322322 is a novel inhibitor of peptide deformylase (PDF) with good in vitro activity against bacteria associated with community-acquired pneumonia and skin infections. "( Pharmacokinetics/Pharmacodynamics of Peptide Deformylase Inhibitor GSK1322322 against Streptococcus pneumoniae, Haemophilus influenzae, and Staphylococcus aureus in Rodent Models of Infection.
Aubart, K; DeMarsh, P; Hoover, J; Lewandowski, T; Novick, SJ; Rittenhouse, S; Straub, RJ; Zalacain, M, 2016)		2.11

Treatment

ExcerptReferenceRelevance
"Treatment with GSK1322322 and linezolid was associated with ≥20% decreases from the baseline in the lesion area in 73% (36/49) and 92% (24/26) of the patients, respectively, at the 48-h assessment and in 96% (44/46) and 100% (25/25) of the patients, respectively, at the 72-h assessment."( Safety, tolerability, and efficacy of GSK1322322 in the treatment of acute bacterial skin and skin structure infections.
Corey, R; Dumont, E; Jones, LS; Kurtinecz, M; Naderer, OJ; O'Riordan, WD; Zhu, JZ, 2014)		1.01

Toxicity

GSK1322322 was generally well tolerated-all adverse events were mild to moderate in intensity. Administration was associated with mild-to-moderate drug-related adverse events. Most commonly, nausea, vomiting, diarrhea, and headache.

ExcerptReferenceRelevance
" GSK1322322 was generally well tolerated, with all adverse events being mild to moderate in intensity during both parts of the study."( Single-dose safety, tolerability, and pharmacokinetics of the antibiotic GSK1322322, a novel peptide deformylase inhibitor.
Dumont, E; Jones, LS; Kurtinecz, M; Naderer, OJ; Zhu, J, 2013)		1.53
" GSK1322322 was generally well tolerated-all adverse events were mild to moderate in intensity."( Safety, tolerability and pharmacokinetics of repeat dosing of the antibiotic GSK1322322, a peptide deformylase inhibitor: a randomized placebo-controlled study.
Dumont, E; Jones, LS; Kurtinecz, M; Naderer, OJ; Zhu, J, 2013)		1.53
" GSK1322322 administration at single and repeat IV doses and at supratherapeutic single IV doses of 2,000 and 3,000 mg was associated with mild-to-moderate drug-related adverse events."( Safety, tolerability, and pharmacokinetics of oral and intravenous administration of GSK1322322, a peptide deformylase inhibitor.
Dumont, E; Jones, LS; Kurtinecz, M; Naderer, OJ; Zhu, J, 2013)		1.52
" GSK1322322 administration was associated with mild-to-moderate drug-related adverse events, most commonly, nausea, vomiting, diarrhea, and headache."( Safety, tolerability, and efficacy of GSK1322322 in the treatment of acute bacterial skin and skin structure infections.
Corey, R; Dumont, E; Jones, LS; Kurtinecz, M; Naderer, OJ; O'Riordan, WD; Zhu, JZ, 2014)		1.58

Pharmacokinetics

There was no age effect or diurnal variation in the GSK1322322 pharmacokinetic profile. This randomized, double-blind, placebo-controlled, eight-cohort phase I trial enrolled 62 healthy volunteers to assess safety and tolerability.

ExcerptReferenceRelevance
" There was no age effect or diurnal variation in the GSK1322322 pharmacokinetic profile."( Safety, tolerability and pharmacokinetics of repeat dosing of the antibiotic GSK1322322, a peptide deformylase inhibitor: a randomized placebo-controlled study.
Dumont, E; Jones, LS; Kurtinecz, M; Naderer, OJ; Zhu, J, 2013)		0.87
" This randomized, double-blind, placebo-controlled, eight-cohort phase I trial enrolled 62 healthy volunteers to assess safety, tolerability, and pharmacokinetic profiles of GSK1322322."( Safety, tolerability, and pharmacokinetics of oral and intravenous administration of GSK1322322, a peptide deformylase inhibitor.
Dumont, E; Jones, LS; Kurtinecz, M; Naderer, OJ; Zhu, J, 2013)		0.81
" aureus using an in vitro pharmacodynamic model and, in parallel, to examine its cellular pharmacokinetics and intracellular disposition."( Cellular pharmacokinetics and intracellular activity of the novel peptide deformylase inhibitor GSK1322322 against Staphylococcus aureus laboratory and clinical strains with various resistance phenotypes: studies with human THP-1 monocytes and J774 murine
Butler, D; Peyrusson, F; Tulkens, PM; Van Bambeke, F, 2015)		0.64
" We have characterized the in vivo pharmacodynamics (PD) of GSK1322322 in immunocompetent animal models of infection with Streptococcus pneumoniae and Haemophilus influenzae (mouse lung model) and with Staphylococcus aureus (rat abscess model) and determined the pharmacokinetic (PK)/PD index that best correlates with efficacy and its magnitude."( Pharmacokinetics/Pharmacodynamics of Peptide Deformylase Inhibitor GSK1322322 against Streptococcus pneumoniae, Haemophilus influenzae, and Staphylococcus aureus in Rodent Models of Infection.
Aubart, K; DeMarsh, P; Hoover, J; Lewandowski, T; Novick, SJ; Rittenhouse, S; Straub, RJ; Zalacain, M, 2016)		0.91
" After the completion of chemical synthesis, all the compounds were evaluated through in vitro antibacterial activity assay, some of which were further subject to in vivo rat pharmacokinetic assessment."( New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
Chen, C; Hu, W; Lv, F; Tang, Y; Wei, J; Zhu, T, 2016)		0.43

Bioavailability

ExcerptReferenceRelevance
" Administration of the drug with a high-fat meal reduced the rate of absorption (reduced C(max) and delayed T(max)) without affecting the extent of absorption (no effect on AUC)."( Single-dose safety, tolerability, and pharmacokinetics of the antibiotic GSK1322322, a novel peptide deformylase inhibitor.
Dumont, E; Jones, LS; Kurtinecz, M; Naderer, OJ; Zhu, J, 2013)		0.62
" After oral tablet doses of GSK1322322 1,000 and 1,500 mg, absolute bioavailability was 69% and 56%, respectively."( Safety, tolerability, and pharmacokinetics of oral and intravenous administration of GSK1322322, a peptide deformylase inhibitor.
Dumont, E; Jones, LS; Kurtinecz, M; Naderer, OJ; Zhu, J, 2013)		0.91
"5 hour; bioavailability 97%)."( Investigation of metabolism and disposition of GSK1322322, a peptidase deformylase inhibitor, in healthy humans using the entero-test for biliary sampling.
Bowen, C; Chen, L; Deng, Y; Dumont, E; Felgate, C; Gorycki, PD; Jones, L; Lin, M; Mamaril-Fishman, D; Naderer, O; Patel, P; Pierre, E; Stump, P; Wen, B; Zhu, J, 2014)		0.66

Dosage Studied

Study provides plasma and intrapulmonary pharmacokinetics, safety, and tolerability of GSK1322322 after repeat (twice daily intravenous dosing for 4 days) dosing at 1,500 mg.

ExcerptRelevanceReference
" Volunteers received a single morning dose of a powder-in-bottle formulation of GSK1322322 or placebo on day 1, no dosing on day 2 and twice-daily dosing on days 3-12."( Safety, tolerability and pharmacokinetics of repeat dosing of the antibiotic GSK1322322, a peptide deformylase inhibitor: a randomized placebo-controlled study.
Dumont, E; Jones, LS; Kurtinecz, M; Naderer, OJ; Zhu, J, 2013)		0.85
" After single dosing of GSK1322322, maximum plasma concentration and exposure (AUC) were dose proportional from 500 to 1500 mg."( Safety, tolerability and pharmacokinetics of repeat dosing of the antibiotic GSK1322322, a peptide deformylase inhibitor: a randomized placebo-controlled study.
Dumont, E; Jones, LS; Kurtinecz, M; Naderer, OJ; Zhu, J, 2013)		0.93
" This report provides plasma and intrapulmonary pharmacokinetics, safety, and tolerability of GSK1322322 after repeat (twice daily intravenous dosing for 4 days) dosing at 1,500 mg."( Penetration of GSK1322322 into epithelial lining fluid and alveolar macrophages as determined by bronchoalveolar lavage.
Bowen, CL; Chen, L; Dumont, E; Jones, LS; Naderer, OJ; Rodvold, KA; Zhu, JZ, 2014)		0.97
" Our study shows that dosing regimen and target class are important factors when considering the impact of antibiotic usage on GI microbiota."( Microbiome changes in healthy volunteers treated with GSK1322322, a novel antibiotic targeting bacterial peptide deformylase.
Arat, S; Aubart, K; Brown, JR; Holmes, DJ; Ingraham, K; Jones, L; Livi, GP; Naderer, O; Sathe, G; Spivak, A; Thomas, E; Traini, C; Van Horn, S, 2015)		0.67
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Peptide deformylaseStaphylococcus aureusIC50 (µMol)0.01200.01200.02070.0300AID1633904
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (42)

Assay IDTitleYearJournalArticle
AID1311230Antibacterial activity against methicillin-sensitive Staphylococcus aureus 14-32016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1633914Solubility of compound by chemiluminescent nitrogen detection assay2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1311241Antibacterial activity against Enterococcus faecalis 14-32016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1633925Oral bioavailability in rat at 8.5 mg/kg2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1311237Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 14-22016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1311242Antibacterial activity against Enterococcus faecalis 14-52016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1311240Antibacterial activity against Enterococcus faecalis 14-22016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1311225Antibacterial activity against methicillin-resistant Staphylococcus aureus 14-22016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1311232Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 14-12016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1633922AUC in rat at 3.9 mg/kg, iv2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1633917Antimicrobial activity against Streptococcus pneumoniae2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1633915Antimicrobial activity against Staphylococcus aureus2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1311233Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 14-22016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1633908Inhibition of Streptococcus pneumoniae PDF by absorbance detection assay2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1311243Antibacterial activity against Escherichia coli 14-12016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1633904Inhibition of Staphylococcus aureus PDF by absorbance detection assay2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1633924AUC in rat at 8.5 mg/kg, po2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1633910Antimicrobial activity against Staphylococcus aureus Oxford2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1633913Chromatographic hydrophobicity index, log D of compound at pH 7.42019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1633921Volume of distribution at steady state in rat at 3.9 mg/kg, iv2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1633920Half life in rat at 8.5 mg/kg, po2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1311236Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 14-12016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1633912Antimicrobial activity against Streptococcus pneumoniae 16292019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1633918Half life in rat at 3.9 mg/kg, iv2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1311224Antibacterial activity against methicillin-resistant Staphylococcus aureus 14-12016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1311235Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 14-42016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1633919Clearance in rat at 3.9 mg/kg, iv2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1311244Antibacterial activity against Escherichia coli 14-22016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1311231Antibacterial activity against methicillin-sensitive Staphylococcus aureus 14-42016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1311227Antibacterial activity against methicillin-resistant Staphylococcus aureus 14-52016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1311234Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 14-32016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1633906Inhibition of Haemophilus influenzae PDF by absorbance detection assay2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1311228Antibacterial activity against methicillin-sensitive Staphylococcus aureus 14-12016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1633911Antimicrobial activity against Haemophilus influenzae Q12019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1311229Antibacterial activity against methicillin-sensitive Staphylococcus aureus 14-22016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1311238Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 14-32016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1633916Antimicrobial activity against Haemophilus influenzae2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
AID1311239Antibacterial activity against Enterococcus faecalis 14-12016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1311246Antibacterial activity against Escherichia coli 14-2 expressing extended-spectrum beta-lactamase2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1311226Antibacterial activity against methicillin-resistant Staphylococcus aureus 14-42016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1311245Antibacterial activity against Escherichia coli 14-1 expressing extended-spectrum beta-lactamase2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1633923Cmax in rat at 8.5 mg/kg, po2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (16)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's16 (100.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.29

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.29 (24.57)
Research Supply Index3.22 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.29)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials8 (50.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (50.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
amoxicillin
Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group.		2.2110penicillin allergen;
penicillin		antibacterial drug
oxazolidin-2-one
Oxazolidinones: Derivatives of oxazolidin-2-one. They represent an important class of synthetic antibiotic agents.. oxazolidin-2-one : An oxazolidinone that is 1,3-oxazolidine with an oxo substituent at position 2.. oxazolidinone : An oxazolidine containing one or more oxo groups.		4.411carbamate ester;
oxazolidinone		metabolite
levofloxacin
Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase.		2.52209-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid;
fluoroquinolone antibiotic;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
linezolid
[no description available]		4.411acetamides;
morpholines;
organofluorine compound;
oxazolidinone		antibacterial drug;
protein synthesis inhibitor
zithromax
Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections.		2.1110macrolide antibioticantibacterial drug;
environmental contaminant;
xenobiotic
nvp pdf 713
[no description available]		2.1310
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		2.1310cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Infections, Respiratory
[description not available]		04.8521
Infectious Skin Diseases
[description not available]		02.2110
Respiratory Tract Infections
Invasion of the host RESPIRATORY SYSTEM by microorganisms, usually leading to pathological processes or diseases.		04.8521
Skin Diseases, Infectious
Skin diseases caused by bacteria, fungi, parasites, or viruses.		02.2110
Bilateral Headache
[description not available]		04.3911
Headache
The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS.		04.3911
Adverse Drug Event
[description not available]		04.3911
Drug-Related Side Effects and Adverse Reactions
Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.		04.3911
Infections, Staphylococcal Skin
[description not available]		04.411
Staphylococcal Skin Infections
Infections to the skin caused by bacteria of the genus STAPHYLOCOCCUS.		04.411
Infections, Legionella pneumophila
[description not available]		02.1110
Haemophilus Infections
Infections with bacteria of the genus HAEMOPHILUS.		02.5220
Infections, Pneumococcal
[description not available]		02.1110
Infections, Staphylococcal
[description not available]		02.5220
Pneumococcal Infections
Infections with bacteria of the species STREPTOCOCCUS PNEUMONIAE.		02.1110
Staphylococcal Infections
Infections with bacteria of the genus STAPHYLOCOCCUS.		02.5220
Pneumonia, Pneumococcal
A febrile disease caused by STREPTOCOCCUS PNEUMONIAE.		02.1310