Evidence map›Paper›PMID 33374964›Full record

ArticlePharmaceutics2020

Hybrid Inhibitors of DNA Gyrase A and B: Design, Synthesis and Evaluation.

Martina Durcik, Žiga Skok, Janez Ilaš, Nace Zidar, Anamarija Zega, Petra Éva Szili, Gábor Draskovits, Tamás Révész, Danijel Kikelj, Akos Nyerges and 3 more

Open access · goldAbstract read
In one paragraph

Article in Pharmaceutics, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.8field-weighted citation impact, top 30% 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

4 citing papers in PubMed, 15 citations in OpenAlex.

  1. Article
  2. Review
  3. Review
  4. 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

13 authors at 3 institutions in 3 countries.

Martina DurcikUniversity of Ljubljana, Faculty of Pharmacy, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.
Žiga SkokUniversity of Ljubljana, Faculty of Pharmacy, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.ORCID 0000-0002-3150-360X
Janez IlašUniversity of Ljubljana, Faculty of Pharmacy, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.ORCID 0000-0002-0124-0474
Nace ZidarUniversity of Ljubljana, Faculty of Pharmacy, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.ORCID 0000-0003-1905-0158
Anamarija ZegaUniversity of Ljubljana, Faculty of Pharmacy, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.
Petra Éva SziliSynthetic and Systems Biology Unit, Institute of Biochemistry, Biological Research Centre, H-6726 Szeged, Hungary.
Gábor DraskovitsSynthetic and Systems Biology Unit, Institute of Biochemistry, Biological Research Centre, H-6726 Szeged, Hungary.
Tamás RévészSynthetic and Systems Biology Unit, Institute of Biochemistry, Biological Research Centre, H-6726 Szeged, Hungary.
Danijel KikeljUniversity of Ljubljana, Faculty of Pharmacy, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.
Akos NyergesSynthetic and Systems Biology Unit, Institute of Biochemistry, Biological Research Centre, H-6726 Szeged, Hungary.ORCID 0000-0002-1581-490X
Csaba PálSynthetic and Systems Biology Unit, Institute of Biochemistry, Biological Research Centre, H-6726 Szeged, Hungary.
Lucija Peterlin MašičUniversity of Ljubljana, Faculty of Pharmacy, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.
Tihomir TomašičUniversity of Ljubljana, Faculty of Pharmacy, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.ORCID 0000-0001-5534-209X
University of Ljubljana · SIHUN-REN Szegedi Biológiai Kutatóközpont · HUHarvard University · US

Funding

Boehringer Ingelheim Fonds A PhD Fellowship for Akos Nyerges'Célzott Lendület' Programme of the Hungarian Academy of Sciences LP-2017-10/2017EFOP EFOP 3.6.3-VEKOP-16-2017-00009'Élvonal' KKP 126506European Research Council H2020-ERC-2014-CoG 648364EVOMER GINOP-2.3.2-15-2016-00014MolMedEx TUMORDNS GINOP-2.3.2-15-2016-00020New National Excellence Programme of the Ministry for Innovation and Technology UNKP-20-3Slovenian Research Agency P1-0208
6 · The paper itself

Abstract

The discovery of multi-targeting ligands of bacterial enzymes is an important strategy to combat rapidly spreading antimicrobial resistance. Bacterial DNA gyrase and topoisomerase IV are validated targets for the development of antibiotics. They can be inhibited at their catalytic sites or at their ATP binding sites. Here we present the design of new hybrids between the catalytic inhibitor ciprofloxacin and ATP-competitive inhibitors that show low nanomolar inhibition of DNA gyrase and antibacterial activity against Gram-negative pathogens. The most potent hybrid

Indexed as

antibacterialciprofloxacinDNA gyrasedual inhibitorhybrid

Identifiers

PMID33374964
PMCPMC7822030
OpenAlexW3116036036

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.