Evidence map›Paper›PMID 35396128›Full record

ArticleBioorganic & medicinal chemistry2022

Synthesis and biological evaluation of imidamide analogs as selective anti-trypanosomal agents.

Viharika Bobba, Yaxin Li, Marjia Afrin, Raina Dano, Wenjing Zhang, Bibo Li, Bin Su

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

Article in Bioorganic & medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.5field-weighted citation impact, top 38% 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

2 citing papers in PubMed, 3 citations in OpenAlex.

  1. Article
  2. 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

7 authors at 1 institution in 1 country.

Viharika BobbaDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Sciences and Health Professions, Cleveland State University, 2121 Euclid Ave., Cleveland, OH, 44115, USA.
Yaxin LiDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Sciences and Health Professions, Cleveland State University, 2121 Euclid Ave., Cleveland, OH, 44115, USA.
Marjia AfrinDepartment of Biological, Geological, and Environmental Sciences, Center for Gene Regulation in Health and Disease, College of Sciences and Health Professions, Cleveland State University, 2121 Euclid Ave., Cleveland, OH, 44115, USA.
Raina DanoDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Sciences and Health Professions, Cleveland State University, 2121 Euclid Ave., Cleveland, OH, 44115, USA.
Wenjing ZhangDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Sciences and Health Professions, Cleveland State University, 2121 Euclid Ave., Cleveland, OH, 44115, USA.
Bibo LiDepartment of Biological, Geological, and Environmental Sciences, Center for Gene Regulation in Health and Disease, College of Sciences and Health Professions, Cleveland State University, 2121 Euclid Ave., Cleveland, OH, 44115, USA. Electronic address: b.li37@csuohio.edu.
Bin SuDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Sciences and Health Professions, Cleveland State University, 2121 Euclid Ave., Cleveland, OH, 44115, USA. Electronic address: b.su@csuohio.edu.
Cleveland State University · US

Funding

Selective tubulin inhibitors with improved cell update for kinetoplastid infectionsR15AI103889 · NIAID · CLEVELAND STATE UNIVERSITY · PI SU, BIN · 2013 to 2016
$873k
A Digital Laser Scanner Biomolecular Imaging System: Amersham Typhoon 5S10OD025252 · OD · CLEVELAND STATE UNIVERSITY · PI LI, BIBO · 2018 to 2018
$163k
NIAID NIH HHS R15 AI103889NIH HHS S10 OD025252
6 · The paper itself

Abstract

Human African trypanosomiasis is caused by a protozoan parasite Trypanosoma brucei majorly infecting people living in sub-Saharan Africa. Current limited available treatments suffer from drug resistance, severe adverse effects, low efficacy, and costly administrative procedures in African countries with limited medical resources. Therefore, there is always a perpetual demand for advanced drug development and invention of new strategies to combat the disease. Previous work in our lab generated a library of sulfonamide analogs as selective tubulin inhibitors, based on the structural difference between mammalian and trypanosome tubulin proteins. Further lead derivatization was performed in the current study and generated 25 potential drug candidates to improve the drug efficacy and uptake by selectively targeting the parasite's P2 membrane transporter protein with imidamide moiety. One of the newly synthesized analogs, compound 25 with a di-imidamide moiety, has shown greater potency with an IC

Indexed as

Trypanocidal AgentsTrypanosoma brucei bruceiTrypanosomiasis, AfricanAnimalsHumansMammalsTubulinTubulin ModulatorsTrypanocidal AgentsTubulinTubulin ModulatorsLead optimizationP2 transporterTrypanosomiasisTubulin inhibitor

Identifiers

PMID35396128
PMCPMC9074797
OpenAlexW4223623032

What OpenQuestion holds

Textmetadata
LicenceTDM
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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.