Evidence map›Paper›PMID 41853228›Full record

ArticleADMET & DMPK2026

Anti-infective macrozones: design, biological evaluation and structure-activity relationships.

Tomislav Jednačak, Višnja Stepanić, Iva Habinovec, Ivana Mikulandra, Kristina Smokrović, Hana Čipčić Paljetak, Mirjana Bukvić, Jelena Parlov Vuković, Ivan Grgičević, Leda Divjak and 2 more

Abstract read
In one paragraph

Article in ADMET & DMPK, 2026. 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
–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

2 citing papers in PubMed.

  1. Heterocycles in Medicinal Chemistry III.Molecules (Basel, Switzerland) · 2026
    Article
  2. 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

12 authors.

Tomislav JednačakDepartment of Chemistry, Faculty of Science, University of Zagreb, Horvatovac 102a, HR-10000 Zagreb, Croatia.ORCID 0000-0003-1620-094X
Višnja StepanićRuđer Bošković Institute, Bijenička cesta 54, HR-10000 Zagreb, Croatia.ORCID 0000-0001-9518-4153
Iva HabinovecDepartment of Chemistry, Faculty of Science, University of Zagreb, Horvatovac 102a, HR-10000 Zagreb, Croatia.ORCID 0009-0009-9925-9293
Ivana MikulandraDepartment of Chemistry, Faculty of Science, University of Zagreb, Horvatovac 102a, HR-10000 Zagreb, Croatia.ORCID 0009-0006-4237-9903
Kristina SmokrovićDepartment of Chemistry, Faculty of Science, University of Zagreb, Horvatovac 102a, HR-10000 Zagreb, Croatia.ORCID 0009-0009-9925-9293
Hana Čipčić PaljetakCenter for Translational and Clinical Research, School of Medicine, University of Zagreb, Šalata 3, HR-10000 Zagreb, Croatia.ORCID 0000-0002-8837-3156
Mirjana BukvićSelvita, Prilaz baruna Filipovića 29, HR-10000 Zagreb, Croatia.ORCID 0000-0002-1035-7981
Jelena Parlov VukovićNMR Centre, Ruđer Bošković Institute, Bijenička cesta 54, HR-10000 Zagreb, Croatia.ORCID 0000-0002-8464-5599
Ivan GrgičevićLabtim Adria d.o.o., Jaruščica 7A, HR-10020 Zagreb, Croatia.ORCID 0009-0009-5708-6363
Leda DivjakDepartment of Chemistry, Faculty of Science, University of Zagreb, Horvatovac 102a, HR-10000 Zagreb, Croatia.ORCID 0009-0006-3797-3799
Klaus ZanggerOrganic and Bioorganic Chemistry, Institute of Chemistry, University of Graz, Heinrichstraße 28 A-8010 Graz, Austria.ORCID 0000-0003-1682-1594
Predrag NovakDepartment of Chemistry, Faculty of Science, University of Zagreb, Horvatovac 102a, HR-10000 Zagreb, Croatia.ORCID 0000-0002-9303-8213

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Background and purpose: To discover novel compounds active against sensitive and resistant bacterial strains, a series of novel azithromycin-thiosemicarbazone conjugates, the macrozones, have been synthesized and their biological activity evaluated with corresponding (quantitative) structure-activity relationship ((Q)SAR) analyses conducted. Experimental approach: A systematic variation of thiosemicarbazone side-chains and coupling at positions 4"-, 3-, and 9a of the azithromycin scaffold has resulted in a novel class of bacterial ribosome inhibitors. Key results: Compared to azithromycin, the activity of 4"-macrozones has shown the greatest improvements against efflux-resistant Conclusion: The results obtained provide a sound basis for guiding further medicinal chemistry efforts toward the discovery of more potent macrolide anti-infectives, with particular emphasis on resistant bacteria that pose a serious threat to human health.

Indexed as

Azithromycin conjugatesbiological activityresistancesynthesisthiosemicarbazones

Identifiers

PMID41853228
PMCPMC12994594

What OpenQuestion holds

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LicenceCC BY
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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.