Evidence map›Paper›PMID 36614785›Full record

ArticleMaterials (Basel, Switzerland)2023

Synthesis and Structure-Activity Relationship of 2,6-Disubstituted Thiosemicarbazone Derivatives of Pyridine as Potential Antituberculosis Agents.

Dagmara Ziembicka, Katarzyna Gobis, Małgorzata Szczesio, Andrzej Olczak, Ewa Augustynowicz-Kopeć, Agnieszka Głogowska, Izabela Korona-Głowniak, Krzysztof Bojanowski

Open access · goldAbstract read
In one paragraph

Article in Materials (Basel, Switzerland), 2023. 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
1.5field-weighted citation impact, top 21% 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, 10 citations in OpenAlex.

  1. Article
  2. The Role of NQO1 in Ovarian Cancer.International journal of molecular sciences · 2023
    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 4 institutions in 2 countries.

Dagmara ZiembickaDepartment of Organic Chemistry, Faculty of Pharmacy, Medical University of Gdańsk, 107 Gen. Hallera Ave, 80-416 Gdansk, Poland.
Katarzyna GobisDepartment of Organic Chemistry, Faculty of Pharmacy, Medical University of Gdańsk, 107 Gen. Hallera Ave, 80-416 Gdansk, Poland.ORCID 0000-0002-9856-9232
Małgorzata SzczesioInstitute of General and Ecological Chemistry, Faculty of Chemistry, Lodz University of Technology, 116 Żeromskiego St, 90-924 Lodz, Poland.ORCID 0000-0002-1611-7938
Andrzej OlczakInstitute of General and Ecological Chemistry, Faculty of Chemistry, Lodz University of Technology, 116 Żeromskiego St, 90-924 Lodz, Poland.ORCID 0000-0002-5433-1767
Ewa Augustynowicz-KopećDepartment of Microbiology, Institute of Tuberculosis and Pulmonary Diseases, 26 Płocka St, 01-138 Warsaw, Poland.ORCID 0000-0001-6162-8748
Agnieszka GłogowskaDepartment of Microbiology, Institute of Tuberculosis and Pulmonary Diseases, 26 Płocka St, 01-138 Warsaw, Poland.
Izabela Korona-GłowniakDepartment of Pharmaceutical Microbiology, Faculty of Pharmacy, Medical University of Lublin, 1 Chodźki St, 20-093 Lublin, Poland.ORCID 0000-0003-1634-0387
Krzysztof BojanowskiSunny BioDiscovery Inc., 972 East Main St, Santa Paula, CA 93060, USA.ORCID 0000-0001-8692-050X
Gdańsk Medical University · PLLodz University of Technology · PLMedical University of Lublin · PLSunny BioDiscovery (United States) · US

Funding

European Union POWR.03.02.00-00-I035/16-00
6 · The paper itself

Abstract

In this study, six new 2,6-disubstituted thiosemicarbazone derivatives of pyridine were synthesized (4−9), and their tuberculostatic activity was evaluated. All of them showed two- to eightfold higher activity (minimum inhibitory concentration (MIC) 0.5−4 µg/mL) against the resistant strain compared with the reference drug. Compounds 5 and 7, which contained the most basic substituents—pyrrolidine and piperidine—in their structure, strongly inhibited the growth of the standard strain (MIC 2 µg/mL). Furthermore, the same derivatives exhibited activity comparable to that of the reference drugs against some types of Gram-positive bacteria (MIC 0.49 µg/mL) and showed no cytotoxicity (IC50 > 50 µg/mL) in HaCaT cells. The zwitterionic structure of each compound was determined using X-ray crystallography. Absorption, distribution, metabolism, and excretion analyses showed that all compounds are good drug candidates. Thus, compounds 5 and 7 were identified as leading structures for further research on antituberculosis drugs with extended effects.

Indexed as

ADMEantimicrobial activitycytotoxic activitypyridinestructure–activity relationshipsynthesisthiosemicarbazonetuberculostatic activityX-ray

Identifiers

PMID36614785
PMCPMC9822072
OpenAlexW4313573664

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.