Evidence map›Paper›PMID 29589443›Full record

ArticleJournal of medicinal chemistry2018

Nanomolar-Potency 1,2,4-Triazoloquinoxaline Inhibitors of the Kidney Urea Transporter UT-A1.

Sujin Lee, Onur Cil, Elena Diez-Cecilia, Marc O Anderson, Alan S Verkman

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
2.5field-weighted citation impact, top 12% 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

10 citing papers in PubMed, 25 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Article
  5. [1,2,4]triazolo[4,3-Molecules (Basel, Switzerland) · 2023
    Article
  6. Article
  7. Article
  8. Synthesis of New Triazolopyrazine Antimalarial Compounds.Molecules (Basel, Switzerland) · 2021
    Article
  9. Article
  10. Urea-aromatic interactions in biology.Biophysical reviews · 2020
    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

5 authors at 2 institutions in 1 country.

Onur Cil
Elena Diez-CeciliaDepartment of Chemistry and Biochemistry , San Francisco State University , San Francisco , California 94132-1722 , United States.
Marc O AndersonDepartment of Chemistry and Biochemistry , San Francisco State University , San Francisco , California 94132-1722 , United States.ORCID 0000-0002-1233-3801
Alan S Verkman
University of California, San Francisco · USSan Francisco State University · US

Funding

SynthesisP30DK072517 · NIDDK · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VERKMAN, ALAN S · 2005 to 2022
$18.1M
Translational Approaches to Develop Drug Therapy for DiarrheaR24DK099803 · NIDDK · JOHNS HOPKINS UNIVERSITY · PI DONOWITZ, MARK · 2014 to 2019
$8.9M
Functional Role of Aquaporins in Eye PhysiologyR01EY013574 · NEI · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VERKMAN, ALAN S · 2002 to 2022
$7.6M
Application of Novel Optical Methods to Cell DynamicsR37EB000415 · NIBIB · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VERKMAN, ALAN S · 2007 to 2016
$4.1M
Urea transport inhibitors as a new class of diureticsR01DK101373 · NIDDK · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VERKMAN, ALAN S · 2014 to 2018
$1.7M
Application of Novel Optical Methods to Cell DynamicsR01EB000415 · NIBIB · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VERKMAN, ALAN S · 2002 to 2006
$1.7M
NEI NIH HHS R01 EY013574NIBIB NIH HHS R01 EB000415NIBIB NIH HHS R37 EB000415NIDDK NIH HHS P30 DK072517NIDDK NIH HHS R01 DK101373NIDDK NIH HHS R24 DK099803
6 · The paper itself

Abstract

Urea transporter A (UT-A) isoforms encoded by the Slc14a2 gene are expressed in kidney tubule epithelial cells, where they facilitate urinary concentration. UT-A1 inhibition is predicted to produce a unique salt-sparing diuretic action in edema and hyponatremia. Here we report the discovery of 1,2,4-triazoloquinoxalines and the analysis of 37 synthesized analogues. The most potent compound, 8ay, containing 1,2,4-triazolo[4,3- a]quinoxaline-substituted benzenesulfonamide linked by an aryl ether, rapidly and reversibly inhibited UT-A1 urea transport by a noncompetitive mechanism with IC

Indexed as

AnimalsDiuresisDiureticsDogsHumansKidneyMadin Darby Canine Kidney CellsMaleMembrane Transport ProteinsModels, MolecularMolecular ConformationMolecular Docking SimulationOsmolar ConcentrationQuinoxalinesRatsRats, WistarDiureticsMembrane Transport ProteinsQuinoxalinesUreaUrea Transporters

Identifiers

PMID29589443
PMCPMC5976253
OpenAlexW2794970377

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.