Evidence map›Paper›PMID 31281021›Full record

ArticleBioorganic & medicinal chemistry letters2019

Synthesis and evaluation of tetrahydropyrazolopyridine inhibitors of anion exchange protein SLC26A4 (pendrin).

Jie S Zhu, Julia Y Lu, Joseph-Anthony Tan, Amber A Rivera, Puay-Wah Phuan, Marina E Shatskikh, Jung-Ho Son, Peter M Haggie, Alan S Verkman, Mark J Kurth

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

Article in Bioorganic & medicinal chemistry letters, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
0.1field-weighted citation impact, top 48% 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

0 citing papers in PubMed, 2 citations in OpenAlex.

No citing paper in PubMed yet.

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 3 institutions in 1 country.

Jie S ZhuDepartment of Chemistry, University of California, Davis, CA 95616, United States.
Julia Y LuDepartment of Chemistry, University of California, Davis, CA 95616, United States.
Joseph-Anthony TanDepartments of Medicine & Physiology, University of California, San Francisco, CA 94143, United States.
Amber A RiveraDepartments of Medicine & Physiology, University of California, San Francisco, CA 94143, United States.
Puay-Wah PhuanDepartments of Medicine & Physiology, University of California, San Francisco, CA 94143, United States.
Marina E ShatskikhDepartment of Chemistry, University of California, Davis, CA 95616, United States.
Jung-Ho SonDepartment of Chemistry, University of California, Davis, CA 95616, United States.
Peter M HaggieDepartments of Medicine & Physiology, University of California, San Francisco, CA 94143, United States.
Alan S VerkmanDepartments of Medicine & Physiology, University of California, San Francisco, CA 94143, United States.
Mark J KurthDepartment of Chemistry, University of California, Davis, CA 95616, United States. Electronic address: mjkurth@ucdavis.edu.
University of California, San Francisco · USUniversity of California, Davis · USUniversity of California System · US

Funding

SynthesisP30DK072517 · NIDDK · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VERKMAN, ALAN S · 2005 to 2022
$18.1M
XENOBIOTICS AND PRIMARY BILIARY CIRRHOSISR01DK067003 · NIDDK · UNIVERSITY OF CALIFORNIA DAVIS · PI GERSHWIN, MERRILL E · 2003 to 2017
$4.4M
Mechanistically based therapeutic strategies in murine primary biliary cholangitisR01DK123262 · NIDDK · UNIVERSITY OF CALIFORNIA AT DAVIS · PI GERSHWIN, MERRILL E · 2020 to 2023
$1.6M
NIDDK NIH HHS P30 DK072517NIDDK NIH HHS R01 DK067003NIDDK NIH HHS R01 DK123262
6 · The paper itself

Abstract

Pendrin is a transmembrane chloride/anion antiporter that is strongly upregulated in the airways in rhinoviral infection, asthma, cystic fibrosis and chronic rhinosinusitis. Based on its role in the regulation of airway surface liquid depth, pendrin inhibitors have potential indications for treatment of inflammatory airways diseases. Here, a completely regioselective route to tetrahydro-pyrazolopyridine pendrin inhibitors based on 1,3-diketone and substituted hydrazine condensation was been developed. Structure-activity relationships at the tetrahydropyridyl nitrogen were investigated using a focused library, establishing the privileged nature of N-phenyl ureas and improving inhibitor potency by greater than 2-fold.

Indexed as

AnimalsMiceMolecular StructurePyrazolesPyridinesRats, Inbred F344Small Molecule LibrariesStructure-Activity RelationshipSulfate TransportersPyrazolesPyridinesSlc26a4 protein, mouseSmall Molecule LibrariesSulfate TransportersAnion transporterPendrinPyrazoleRegioselectivitySLC26A4

Identifiers

PMID31281021
PMCPMC6690761
OpenAlexW2955714809

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.