Evidence map›Paper›PMID 37984297›Full record

ArticleEuropean journal of medicinal chemistry2024

Discovery of an orally active nitrothiophene-based antitrypanosomal agent.

Oluwatomi Ajayi, Damilohun S Metibemu, Olamide Crown, Olawale S Adeyinka, Marcel Kaiser, Nathalie Shoji, Mariana Silva, Ana Rodriguez, Ifedayo Victor Ogungbe

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

Article in European journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
0.2field-weighted citation impact, top 39% 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

1 citing paper in PubMed, 1 citations in OpenAlex.

  1. Discovery of Strong 3-Nitro-2-Phenyl-International journal of molecular sciences · 2024
    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

9 authors at 4 institutions in 2 countries.

Oluwatomi AjayiDepartment of Chemistry, Physics, and Atmospheric Sciences, Jackson State University, Jackson, MS, 39217, USA.
Damilohun S MetibemuDepartment of Chemistry, Physics, and Atmospheric Sciences, Jackson State University, Jackson, MS, 39217, USA; Department of Chemistry, The University of Alabama in Huntsville, Huntsville, AL, 35899, USA.
Olamide CrownDepartment of Chemistry, Physics, and Atmospheric Sciences, Jackson State University, Jackson, MS, 39217, USA; Department of Chemistry, The University of Alabama in Huntsville, Huntsville, AL, 35899, USA.
Olawale S AdeyinkaDepartment of Chemistry, Physics, and Atmospheric Sciences, Jackson State University, Jackson, MS, 39217, USA; Department of Chemistry, The University of Alabama in Huntsville, Huntsville, AL, 35899, USA.
Marcel KaiserSwiss Tropical and Public Health Institute, Kreuzstrasse 2, 4123, Allschwil, Switzerland; University of Basel, 4001, Basel, Switzerland.
Nathalie ShojiDepartment of Microbiology, New York University Grossman School of Medicine, New York, NY, 10010, USA.
Mariana SilvaUniversity of Basel, 4001, Basel, Switzerland.
Ana RodriguezDepartment of Microbiology, New York University Grossman School of Medicine, New York, NY, 10010, USA.
Ifedayo Victor OgungbeDepartment of Chemistry, Physics, and Atmospheric Sciences, Jackson State University, Jackson, MS, 39217, USA; Department of Chemistry, The University of Alabama in Huntsville, Huntsville, AL, 35899, USA. Electronic address: victor.ogungbe@uah.edu.
Jackson State University · USNew York University · USSwiss Tropical and Public Health Institute · CHUniversity of Basel · CH

Funding

Lead Optimization and Mechanisms of Action of Dual-Acting Antitrypanosomal AgentsSC1GM140990 · NIGMS · JACKSON STATE UNIVERSITY · PI OGUNGBE, IFEDAYO VICTOR · 2021 to 2023
$1.1M
NIGMS NIH HHS SC1 GM140990
6 · The paper itself

Abstract

Human African Trypanosomiasis (HAT), caused by Trypanosoma brucei gambiense and rhodesiense, is a parasitic disease endemic to sub-Saharan Africa. Untreated cases of HAT can be severely debilitating and fatal. Although the number of reported cases has decreased progressively over the last decade, the number of effective and easily administered medications is very limited. In this work, we report the antitrypanosomal activity of a series of potent compounds. A subset of molecules in the series are highly selective for trypanosomes and are metabolically stable. One of the compounds, (E)-N-(4-(methylamino)-4-oxobut-2-en-1-yl)-5-nitrothiophene-2-carboxamide (10), selectively inhibited the growth of T. b. brucei, T. b. gambiense and T. b. rhodesiense, have excellent oral bioavailability and was effective in treating acute infection of HAT in mouse models. Based on its excellent bioavailability, compound 10 and its analogs are candidates for lead optimization and pre-clinical investigations.

Indexed as

Trypanocidal AgentsTrypanosoma brucei bruceiTrypanosomiasis, AfricanAnimalsHumansMiceTrypanosoma brucei gambienseTrypanosoma brucei rhodesienseTrypanocidal AgentsCysteine proteaseHATInhibitorsTrypanosomesVinyl sulfone

Identifiers

PMID37984297
PMCPMC10843616
OpenAlexW4388694814

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.