Evidence map›Paper›PMID 40903488›Full record

ArticleThe Journal of antibiotics2025

Antimicrobial activity of triphenylphosphonium (TPP) conjugates of alkynyl-substituted nucleic bases and their analogues.

Olga V Andreeva, Alexandra D Voloshina, Anna P Lyubina, Bulat F Garifullin, Irina Yu Strobykina, Mayya G Belenok, Olga B Babaeva, Vasily M Babaev, Ravil F Aznagulov, Liliya F Saifina and 2 more

Abstract read
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Article in The Journal of antibiotics, 2025. 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.

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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

12 authors.

Olga V AndreevaArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation.ORCID 0000-0001-5518-8395
Alexandra D VoloshinaArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation. sobaka-1968@mail.ru.ORCID 0000-0002-3540-8554
Anna P LyubinaArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation.
Bulat F GarifullinArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation.
Irina Yu StrobykinaArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation.
Mayya G BelenokArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation.
Olga B BabaevaArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation.
Vasily M BabaevArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation.
Ravil F AznagulovArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation.
Liliya F SaifinaArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation.
Vyacheslav E SemenovArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation.
Vladimir E KataevArbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation.

Funding

Russian Science Foundation (RSF) grant no. 24-13-00006
6 · The paper itself

Abstract

Twenty triphenylphosphonium (TPP) conjugates in which 1-alkynyl-substituted nucleic bases (uracil, thymine) and their analogues (6-methyluracil, quinazoline-2,4-dione) were connected to the TPP cation via an octyl or decyl linker were synthesized. In vitro evaluation of their antibacterial activity against five Gram-positive bacteria, two Gram-negative bacteria and fungus C. albicans revealed six lead compounds which exhibited high bacteriostatic activity (MIC 0.2-0.9 μM) against Gram-positive bacteria S. aureus, B. cereus, E. faecalis, as well as MRSA strains. These lead compounds are TPP-conjugates in which 1-alkynylquinazoline-2,4-dione moiety is bound to the TPP cation via the decyl (4 d, 4 f) or octyl (4e) linker and biscationic TPP-conjugates in which two TPP cations are attached to the N-1 and N-3 atoms of 5-alkynylquinazoline-2,4-dione moiety via the decyl (5 d, 5 f) or octyl (5e) linkers. Biscations 5 d and 5e showed high in vitro bacteriostatic and bactericidal activity (MIC/MBC 0.2-7.8 μM) against Gram-negative bacteria E. coli and P. aeruginosa. In addition, biscations 5 d and 5 f exhibited noticeable in vitro fungistatic and fungicidal activity against fungus C. albicans. Using colorimetric and fluorimetric methods, it was found that all lead compounds at concentrations corresponding to the MIC and MBC values caused cytoplasmic membrane damage and depolarization, without violating the integrity of the S. aureus cell wall. In addition, all lead compounds inhibited the formation of S. aureus biofilm by 80-100% at concentrations close to the MBC value (about 0.8 μM), and destroyed already formed S. aureus biofilm at concentrations in the range of 6.3-12.5 μM.

Indexed as

Anti-Bacterial AgentsOrganophosphorus CompoundsAntifungal AgentsCandida albicansGram-Negative BacteriaGram-Positive BacteriaMicrobial Sensitivity TestsStructure-Activity RelationshipThymineUracilAnti-Bacterial AgentsAntifungal AgentsOrganophosphorus CompoundsThyminetriphenylphosphoniumUracil

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Registered trials

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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.