Evidence map›Paper›PMID 25211002›Full record

ArticleMolecules (Basel, Switzerland)2014

1,2-substituted 4-(1H)-quinolones: synthesis, antimalarial and antitrypanosomal activities in vitro.

Abraham Wube, Antje Hüfner, Werner Seebacher, Marcel Kaiser, Reto Brun, Rudolf Bauer, Franz Bucar

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2014. 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
1.6field-weighted citation impact, top 15% 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, 18 citations in OpenAlex.

  1. Review
  2. Potent Antimalarial 2-Pyrazolyl QuinoloneACS medicinal chemistry letters · 2018
    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

7 authors at 3 institutions in 2 countries.

Abraham WubeDepartment of Pharmacognosy, Institute of Pharmaceutical Sciences, University of Graz, Universitätsplatz 4/1, A-8010 Graz, Austria. abraham.wube@uni-graz.at.
Antje HüfnerDepartment of Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, University of Graz, Universitätsplatz 1, A-8010 Graz, Austria. antje.huefner@uni-graz.at.
Werner SeebacherDepartment of Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, University of Graz, Universitätsplatz 1, A-8010 Graz, Austria. we.seebacher@uni-graz.at.
Marcel KaiserSwiss Tropical and Public Health Institute, Socinstrasse 57, CH-4002 Basel, Switzerland. Marcel.Kaiser@unibas.ch.
Reto BrunSwiss Tropical and Public Health Institute, Socinstrasse 57, CH-4002 Basel, Switzerland. reto.brun@unibas.ch.
Rudolf BauerDepartment of Pharmacognosy, Institute of Pharmaceutical Sciences, University of Graz, Universitätsplatz 4/1, A-8010 Graz, Austria. rudolf.bauer@uni-graz.at.
Franz BucarDepartment of Pharmacognosy, Institute of Pharmaceutical Sciences, University of Graz, Universitätsplatz 4/1, A-8010 Graz, Austria. franz.bucar@uni-graz.at.
University of Graz · ATSwiss Tropical and Public Health Institute · CHUniversity of Basel · CH

Funding

Austrian Science Fund FWF P 24324
6 · The paper itself

Abstract

A diverse array of 4-(1H)-quinolone derivatives bearing substituents at positions 1 and 2 were synthesized and evaluated for antiprotozoal activities against Plasmodium falciparum and Trypanosoma brucei rhodesiense, and cytotoxicity against L-6 cells in vitro. Furthermore, selectivity indices were also determined for both parasites. All compounds tested showed antimalarial activity at low micromolar concentrations, with varied degrees of selectivity against L-6 cells. Compound 5a was found to be the most active against P. falciparum, with an IC50 value of 90 nM and good selectivity for the malarial parasite compared to the L-6 cells. Compound 10a, on the other hand, showed a strong antitrypanosomal effect with an IC50 value of 1.25 µM. In this study side chain diversity was explored by varying the side chain length and substitution pattern on the aliphatic group at position-2 and a structure-antiprotozoal activity study revealed that the aromatic ring introduced at C-2 contributed significantly to the antiprotozoal activities.

Indexed as

AcetylationAnimalsAntimalarialsCell LineDrug Evaluation, PreclinicalInhibitory Concentration 50Parasitic Sensitivity TestsPlasmodium falciparumQuinolonesRatsTrypanocidal AgentsTrypanosoma brucei rhodesienseAntimalarialsQuinolonesTrypanocidal Agents

Identifiers

PMID25211002
PMCPMC6271202
OpenAlexW2117574275

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.