Evidence map›Paper›PMID 30949901›Full record

ArticleMolecular diversity2020

Identification of pyrrolo-pyridine derivatives as novel class of antibacterials.

Mark S Veselov, Yan A Ivanenkov, Renat S Yamidanov, Ilya A Osterman, Petr V Sergiev, Vladimir A Aladinskiy, Anastasia V Aladinskaya, Victor A Terentiev, Andrey A Ayginin, Dmitry A Skvortsov and 15 more

Abstract read
PubMed Publisher
In one paragraph

Article in Molecular diversity, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
–field-weighted citation impact
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

3 citing papers in PubMed.

  1. Review
  2. Review
  3. An Overview of the Biological Activity of Pyrrolo[3,4-Pharmaceuticals (Basel, Switzerland) · 2021
    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

25 authors.

Mark S VeselovInstitute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054. mark.veselov@phystech.edu.
Yan A IvanenkovInstitute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054.
Renat S YamidanovInstitute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054.
Ilya A OstermanChemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3 GSP-1, Moscow, Russian Federation, 119991.
Petr V SergievDepartment of Chemistry and A.N. Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russian Federation.
Vladimir A AladinskiyMoscow Institute of Physics and Technology (State University), 9 Institutskiy Lane, Dolgoprudny City, Moscow Region, Russian Federation, 141700.
Anastasia V AladinskayaMoscow Institute of Physics and Technology (State University), 9 Institutskiy Lane, Dolgoprudny City, Moscow Region, Russian Federation, 141700.
Victor A TerentievInstitute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054.
Andrey A AygininInstitute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054.
Dmitry A SkvortsovDepartment of Chemistry and A.N. Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russian Federation.
Katerina S KomarovaDepartment of Chemistry and A.N. Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russian Federation.
Alexey V ChemerisInstitute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054.
Alexey Kh BaimievInstitute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054.
Alina A SofronovaFaculty of Bioengineering and Bioinformatics, Lomonosov Moscow State University, Moscow, Russian Federation.
Alexey E MachulkinChemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3 GSP-1, Moscow, Russian Federation, 119991.
Rostislav A PetrovChemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3 GSP-1, Moscow, Russian Federation, 119991.
Svetlana Yu MaklakovaChemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3 GSP-1, Moscow, Russian Federation, 119991.
Dmitry S BezrukovSkolkovo Institute of Science and Technology, Skolkovo, Russian Federation.
Gleb I FilkovMoscow Institute of Physics and Technology (State University), 9 Institutskiy Lane, Dolgoprudny City, Moscow Region, Russian Federation, 141700.
Liana F ZainullinaInstitute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054.
Marina A MaximovaInstitute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054.
Zulfiya R ZileevaInstitute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054.
Victor G KartsevInterBioScreen Ltd, Chernogolovka, Moscow Region, Russian Federation.
Yulia V VakhitovaInstitute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054.
Olga A DontsovaChemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3 GSP-1, Moscow, Russian Federation, 119991.

Funding

Ministry of Education and Science of the Russian Federation 20.9907.2017/VURussian Science Foundation №17-74-30012
6 · The paper itself

Abstract

A series of 5-oxo-4H-pyrrolo[3,2-b]pyridine derivatives was identified as novel class of highly potent antibacterial agents during an extensive large-scale high-throughput screening (HTS) program utilizing a unique double-reporter system-pDualrep2. The construction of the reporter system allows us to perform visual inspection of the underlying mechanism of action due to two genes-Katushka2S and RFP-which encode the proteins with different imaging signatures. Antibacterial activity of the compounds was evaluated during the initial HTS round and subsequent rescreen procedure. The most active molecule demonstrated a MIC value of 3.35 µg/mL against E. coli with some signs of translation blockage (low Katushka2S signal) and no SOS response. The compound did not demonstrate cytotoxicity in standard cell viability assay. Subsequent structural morphing and follow-up synthesis may result in novel compounds with a meaningful antibacterial potency which can be reasonably regarded as an attractive starting point for further in vivo investigation and optimization.

Indexed as

Anti-Bacterial AgentsCell SurvivalDrug Evaluation, PreclinicalHigh-Throughput Screening AssaysIndolizinesMicrobial Sensitivity TestsPyridinesStructure-Activity RelationshipAnti-Bacterial AgentsindolizineIndolizinesPyridinesAntibacterial compoundsAntibioticsHTSMICRibosomeSOS responseTranslation inhibition

Identifiers

What OpenQuestion holds

Textmetadata
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.