Evidence map›Paper›PMID 32926544›Full record

ArticleChemMedChem2021

Further SAR on the (Phenylsulfonyl)piperazine Scaffold as Inhibitors of the Aedes aegypti Kir1 (AeKir) Channel and Larvicides.

Christopher D Aretz, Sujay V Kharade, Keagan Chronister, Renata Rusconi Trigueros, Erick J Martinez Rodriguez, Peter M Piermarini, Jerod S Denton, Corey R Hopkins

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

Article in ChemMedChem, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.5field-weighted citation impact, top 28% 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

3 citing papers in PubMed, 7 citations in OpenAlex.

  1. Article
  2. Article
  3. 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

8 authors at 3 institutions in 1 country.

Christopher D AretzDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, 986125 Nebraska Medical Center, Omaha, NE 68198-6125, USA.
Sujay V KharadeDepartment of Anesthesiology, Vanderbilt University Medical Center, T-4208 Medical Center North, Nashville, TN 37232, USA.
Keagan ChronisterDepartment of Anesthesiology, Vanderbilt University Medical Center, T-4208 Medical Center North, Nashville, TN 37232, USA.
Renata Rusconi TriguerosDepartment of Entomology, Ohio State University, 1680 Madison Avenue, Wooster, OH 44691, USA.
Erick J Martinez RodriguezDepartment of Entomology, Ohio State University, 1680 Madison Avenue, Wooster, OH 44691, USA.
Peter M PiermariniDepartment of Entomology, Ohio State University, 1680 Madison Avenue, Wooster, OH 44691, USA.
Jerod S DentonDepartment of Anesthesiology, Vanderbilt University Medical Center, T-4208 Medical Center North, Nashville, TN 37232, USA.
Corey R HopkinsDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, 986125 Nebraska Medical Center, Omaha, NE 68198-6125, USA.ORCID 0000-0003-4958-1697
The Ohio State University · USVanderbilt University Medical Center · USNebraska Medical Center · US

Funding

Development of small molecule mosquitocides for controlling the primary vector of Zika virus, Aedes aegyptiR21AI128418 · NIAID · OHIO STATE UNIVERSITY · PI DENTON, JEROD S., HOPKINS, COREY R. · 2017 to 2018
$448k
NIAID NIH HHS R21 AI128418
6 · The paper itself

Abstract

Zika virus (ZIKV), dengue fever (DENV) and chikungunya (CHIKV) are arboviruses that are spread to humans from the bite of an infected adult female Aedes aegypti mosquito. As there are no effective vaccines or therapeutics for these diseases, the primary strategy for controlling the spread of these viruses is to prevent the mosquito from biting humans through the use of insecticides. Unfortunately, the commonly used classes of insecticides have seen a significant increase in resistance, thus complicating control efforts. Inhibiting the renal inward rectifier potassium (Kir) channel of the mosquito vector Aedes aegypti has been shown to be a promising target for the development of novel mosquitocides. We have shown that Kir1 channels play key roles in mosquito diuresis, hemolymph potassium homeostasis, flight, and reproduction. Previous work from our laboratories identified a novel (phenylsulfonyl)piperazine scaffold as potent AeKir channel inhibitors with activity against both adult and larval mosquitoes. Herein, we report further SAR work around this scaffold and have identified additional compounds with improved in vitro potency and mosquito larvae toxicity.

Indexed as

AedesAnimalsCulicidaeLarvaPiperazineStructure-Activity RelationshipPiperazineAedes aegyptiKir channelslarvae toxicityvector-borne diseasesZika

Identifiers

PMID32926544
PMCPMC7856040
OpenAlexW3087439296

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.