Evidence map›Paper›PMID 25438766›Full record

ArticleBioorganic & medicinal chemistry2014

Inhibition of myeloperoxidase: evaluation of 2H-indazoles and 1H-indazolones.

Aaron Roth, Sean Ott, Kelli M Farber, Teresa A Palazzo, Wayne E Conrad, Makhluf J Haddadin, Dean J Tantillo, Carroll E Cross, Jason P Eiserich, Mark J Kurth

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

Article in Bioorganic & medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
0.9field-weighted citation impact, top 27% 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

7 citing papers in PubMed, 24 citations in OpenAlex.

  1. Article
  2. Electrochemical synthesis ofChemical science · 2022
    Article
  3. 29th Annual GP2A Medicinal Chemistry Conference.Pharmaceuticals (Basel, Switzerland) · 2021
    Article
  4. Review
  5. Article
  6. Article
  7. From Dynamic Combinatorial Chemistry toACS medicinal chemistry letters · 2017
    Article
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

10 authors at 2 institutions in 2 countries.

Aaron RothDepartment of Chemistry, University of California, One Shields Avenue, Davis, CA 95616, United States.
Sean OttDepartment of Internal Medicine, Division of Pulmonary/Critical Care Medicine, 4150 V Street, Suite 3100, Sacramento, CA 95817, United States.
Kelli M FarberDepartment of Chemistry, University of California, One Shields Avenue, Davis, CA 95616, United States.
Teresa A PalazzoDepartment of Chemistry, University of California, One Shields Avenue, Davis, CA 95616, United States.
Wayne E ConradDepartment of Chemistry, University of California, One Shields Avenue, Davis, CA 95616, United States.
Makhluf J HaddadinDepartment of Chemistry, American University of Beirut, Beirut, Lebanon.
Dean J TantilloDepartment of Chemistry, University of California, One Shields Avenue, Davis, CA 95616, United States.
Carroll E CrossDepartment of Internal Medicine, Division of Pulmonary/Critical Care Medicine, 4150 V Street, Suite 3100, Sacramento, CA 95817, United States.
Jason P EiserichDepartment of Internal Medicine, Division of Pulmonary/Critical Care Medicine, 4150 V Street, Suite 3100, Sacramento, CA 95817, United States.
Mark J KurthDepartment of Chemistry, University of California, One Shields Avenue, Davis, CA 95616, United States. Electronic address: mjkurth@ucdavis.edu.
University of California, Davis · USAmerican University of Beirut · LB

Funding

SynthesisP30DK072517 · NIDDK · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VERKMAN, ALAN S · 2005 to 2022
$18.1M
Complex Heterocycles and Hybrid Strategies for Pilot Scale LibrariesP41GM089153 · NIGMS · UNIVERSITY OF CALIFORNIA AT DAVIS · PI KURTH, MARK J. · 2010 to 2012
$1.1M
Therapeutic Targeting of Myeloperoxidase in Acute InflammationR21HL092506 · NHLBI · UNIVERSITY OF CALIFORNIA AT DAVIS · PI CROSS, CARROLL E · 2009 to 2011
$416k
NHLBI NIH HHS HL092506NHLBI NIH HHS R21 HL092506NIDDK NIH HHS DK72517NIDDK NIH HHS P30 DK072517NIGMS NIH HHS GM089153NIGMS NIH HHS P41 GM089153
6 · The paper itself

Abstract

Myeloperoxidase (MPO) produces hypohalous acids as a key component of the innate immune response; however, release of these acids extracellularly results in inflammatory cell and tissue damage. The two-step, one-pot Davis-Beirut reaction was used to synthesize a library of 2H-indazoles and 1H-indazolones as putative inhibitors of MPO. A structure-activity relationship study was undertaken wherein compounds were evaluated utilizing taurine-chloramine and MPO-mediated H2O2 consumption assays. Docking studies as well as toxicophore and Lipinski analyses were performed. Fourteen compounds were found to be potent inhibitors with IC50 values <1μM, suggesting these compounds could be considered as potential modulators of pro-oxidative tissue injury pertubated by the inflammatory MPO/H2O2/HOCl/HOBr system.

Indexed as

Binding SitesCatalytic DomainChloraminesHumansIndazolesMolecular Docking SimulationPeroxidaseProtein BindingStructure-Activity RelationshipTaurinechloramineChloraminesIndazolesPeroxidaseTaurine2H-IndazoleComputational dockingDavis–Beirut reactionMyeloperoxidaseStructure–activity relationship

Identifiers

PMID25438766
PMCPMC4254468
OpenAlexW1991646087

What OpenQuestion holds

Textmetadata
LicenceTDM
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.