Evidence map›Paper›PMID 31201212›Full record

ArticleDrug metabolism and disposition: the biological fate of chemicals2019

Structure-Guided In Vitro to In Vivo Pharmacokinetic Optimization of Propargyl-Linked Antifolates.

M N Lombardo, N G-Dayanandan, S Keshipeddy, W Zhou, D Si, S M Reeve, J Alverson, P Barney, L Walker, J Hoody and 3 more

Open access · hybridAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Drug metabolism and disposition: the biological fate of chemicals, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.3field-weighted citation impact, top 47% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

4 citing papers in PubMed, 8 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

13 authors at 1 institution in 1 country.

M N LombardoDepartment of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut (M.N.L., N.G.-D., S.K., W.Z., D.S., S.M.R., D.L.W.); Pfizer Worldwide Research & Development, Pharmacokinetics, Dynamics, and Metabolism, Groton, Connecticut (R.S.O.); and Department of Chemistry and Biochemistry, University of Montana, Missoula, Montana (J.A., P.B., L.W., J.H., N.D.P.).ORCID 0000-0002-4239-8630
N G-DayanandanDepartment of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut (M.N.L., N.G.-D., S.K., W.Z., D.S., S.M.R., D.L.W.); Pfizer Worldwide Research & Development, Pharmacokinetics, Dynamics, and Metabolism, Groton, Connecticut (R.S.O.); and Department of Chemistry and Biochemistry, University of Montana, Missoula, Montana (J.A., P.B., L.W., J.H., N.D.P.).
S KeshipeddyDepartment of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut (M.N.L., N.G.-D., S.K., W.Z., D.S., S.M.R., D.L.W.); Pfizer Worldwide Research & Development, Pharmacokinetics, Dynamics, and Metabolism, Groton, Connecticut (R.S.O.); and Department of Chemistry and Biochemistry, University of Montana, Missoula, Montana (J.A., P.B., L.W., J.H., N.D.P.).
W ZhouDepartment of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut (M.N.L., N.G.-D., S.K., W.Z., D.S., S.M.R., D.L.W.); Pfizer Worldwide Research & Development, Pharmacokinetics, Dynamics, and Metabolism, Groton, Connecticut (R.S.O.); and Department of Chemistry and Biochemistry, University of Montana, Missoula, Montana (J.A., P.B., L.W., J.H., N.D.P.).ORCID 0000-0002-9375-2230
D SiDepartment of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut (M.N.L., N.G.-D., S.K., W.Z., D.S., S.M.R., D.L.W.); Pfizer Worldwide Research & Development, Pharmacokinetics, Dynamics, and Metabolism, Groton, Connecticut (R.S.O.); and Department of Chemistry and Biochemistry, University of Montana, Missoula, Montana (J.A., P.B., L.W., J.H., N.D.P.).
S M ReeveDepartment of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut (M.N.L., N.G.-D., S.K., W.Z., D.S., S.M.R., D.L.W.); Pfizer Worldwide Research & Development, Pharmacokinetics, Dynamics, and Metabolism, Groton, Connecticut (R.S.O.); and Department of Chemistry and Biochemistry, University of Montana, Missoula, Montana (J.A., P.B., L.W., J.H., N.D.P.).
J AlversonDepartment of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut (M.N.L., N.G.-D., S.K., W.Z., D.S., S.M.R., D.L.W.); Pfizer Worldwide Research & Development, Pharmacokinetics, Dynamics, and Metabolism, Groton, Connecticut (R.S.O.); and Department of Chemistry and Biochemistry, University of Montana, Missoula, Montana (J.A., P.B., L.W., J.H., N.D.P.).
P BarneyDepartment of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut (M.N.L., N.G.-D., S.K., W.Z., D.S., S.M.R., D.L.W.); Pfizer Worldwide Research & Development, Pharmacokinetics, Dynamics, and Metabolism, Groton, Connecticut (R.S.O.); and Department of Chemistry and Biochemistry, University of Montana, Missoula, Montana (J.A., P.B., L.W., J.H., N.D.P.).
L WalkerDepartment of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut (M.N.L., N.G.-D., S.K., W.Z., D.S., S.M.R., D.L.W.); Pfizer Worldwide Research & Development, Pharmacokinetics, Dynamics, and Metabolism, Groton, Connecticut (R.S.O.); and Department of Chemistry and Biochemistry, University of Montana, Missoula, Montana (J.A., P.B., L.W., J.H., N.D.P.).
J HoodyDepartment of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut (M.N.L., N.G.-D., S.K., W.Z., D.S., S.M.R., D.L.W.); Pfizer Worldwide Research & Development, Pharmacokinetics, Dynamics, and Metabolism, Groton, Connecticut (R.S.O.); and Department of Chemistry and Biochemistry, University of Montana, Missoula, Montana (J.A., P.B., L.W., J.H., N.D.P.).
N D PriestleyDepartment of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut (M.N.L., N.G.-D., S.K., W.Z., D.S., S.M.R., D.L.W.); Pfizer Worldwide Research & Development, Pharmacokinetics, Dynamics, and Metabolism, Groton, Connecticut (R.S.O.); and Department of Chemistry and Biochemistry, University of Montana, Missoula, Montana (J.A., P.B., L.W., J.H., N.D.P.).
R S ObachDepartment of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut (M.N.L., N.G.-D., S.K., W.Z., D.S., S.M.R., D.L.W.); Pfizer Worldwide Research & Development, Pharmacokinetics, Dynamics, and Metabolism, Groton, Connecticut (R.S.O.); and Department of Chemistry and Biochemistry, University of Montana, Missoula, Montana (J.A., P.B., L.W., J.H., N.D.P.).
D L WrightDepartment of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut (M.N.L., N.G.-D., S.K., W.Z., D.S., S.M.R., D.L.W.); Pfizer Worldwide Research & Development, Pharmacokinetics, Dynamics, and Metabolism, Groton, Connecticut (R.S.O.); and Department of Chemistry and Biochemistry, University of Montana, Missoula, Montana (J.A., P.B., L.W., J.H., N.D.P.) dennis.wright@uconn.edu.ORCID 0000-0003-4634-3351
University of Connecticut · US

Funding

Propargyl-linked Antifolates Targeting Klebsiella pneumoniaeR01AI104841 · NIAID · UNIVERSITY OF CONNECTICUT STORRS · PI WRIGHT, DENNIS L. · 2014 to 2018
$3.1M
Antimetabolites Effective against Resistant Gram-positive BacteriaR01AI111957 · NIAID · UNIVERSITY OF CONNECTICUT STORRS · PI WRIGHT, DENNIS L. · 2014 to 2017
$2.2M
NIAID NIH HHS R01 AI104841NIAID NIH HHS R01 AI111957
6 · The paper itself

Abstract

Pharmacokinetic/pharmacodynamic properties are strongly correlated with the in vivo efficacy of antibiotics. Propargyl-linked antifolates, a novel class of antibiotics, demonstrate potent antibacterial activity against both Gram-positive and Gram-negative pathogenic bacteria, including multidrug-resistant

Indexed as

Drug DesignModels, BiologicalAnimalsAnti-Bacterial AgentsBacterial ProteinsCell LineCrystallography, X-RayCytochrome P-450 CYP3ADrug InteractionsDrug Resistance, BacterialEnzyme AssaysFemaleFolic Acid AntagonistsHepatocytesHumansInhibitory Concentration 50Anti-Bacterial AgentsBacterial ProteinsCYP3A4 protein, humanCytochrome P-450 CYP3AFolic Acid AntagonistsRecombinant ProteinsTetrahydrofolate Dehydrogenase

Identifiers

PMID31201212
PMCPMC7184189
OpenAlexW2952435022

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.