Evidence map›Paper›PMID 40726219›Full record

ArticleArchiv der Pharmazie2025

Design and Synthesis of Ketoconazole Derivatives as Innovative Anti-Infective Agents.

Gioele Renzi, Andrea Angeli, Silvia Selleri, Costanza Spadini, Nicolo' Mezzasalma, Marcus T Hull, Steven L Kelly, Clemente Capasso, Clotilde S Cabassi, Fabrizio Carta and 1 more

Abstract read
In one paragraph

Article in Archiv der Pharmazie, 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.

  1. Review
  2. Article
  3. 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

11 authors.

Gioele RenziNEUROFARBA Department, Section of Pharmaceutical and Nutraceutical Sciences, Sesto Fiorentino, Università degli Studi di Firenze, Florence, Italy.ORCID https://orcid.org/0009-0008-9109-030X
Andrea AngeliNEUROFARBA Department, Section of Pharmaceutical and Nutraceutical Sciences, Sesto Fiorentino, Università degli Studi di Firenze, Florence, Italy.ORCID https://orcid.org/0000-0002-1470-7192
Silvia SelleriNEUROFARBA Department, Section of Pharmaceutical and Nutraceutical Sciences, Sesto Fiorentino, Università degli Studi di Firenze, Florence, Italy.
Costanza SpadiniDepartment of Veterinary Science, University of Parma, Parma, Italy.ORCID https://orcid.org/0000-0003-0211-5293
Nicolo' MezzasalmaDepartment of Veterinary Science, University of Parma, Parma, Italy.
Marcus T HullFaculty of Medicine, Health and Life Science, Institute of Life Science, Swansea University, Swansea, UK.
Steven L KellyFaculty of Medicine, Health and Life Science, Institute of Life Science, Swansea University, Swansea, UK.
Clemente CapassoDepartment of Biology, Agriculture and Food Sciences, Institute of Biosciences and Bioresources, Napoli, Italy.
Clotilde S CabassiDepartment of Veterinary Science, University of Parma, Parma, Italy.ORCID https://orcid.org/0000-0002-1936-9858
Fabrizio CartaNEUROFARBA Department, Section of Pharmaceutical and Nutraceutical Sciences, Sesto Fiorentino, Università degli Studi di Firenze, Florence, Italy.ORCID https://orcid.org/0000-0002-1141-6146
Claudiu T SupuranNEUROFARBA Department, Section of Pharmaceutical and Nutraceutical Sciences, Sesto Fiorentino, Università degli Studi di Firenze, Florence, Italy.ORCID https://orcid.org/0000-0003-4262-0323

Funding

F.C. was grateful to Ente Cassa di Risparmio di Firenze for partially supporting this work. Project title "Progettazione e Sintesi di Nuovi Agenti per la Cura e la Profilassi di Infezioni Batteriche Resistenti". CRF 2018.1001.
6 · The paper itself

Abstract

A novel series of compounds was designed and synthesized by combining the distal piperazine nitrogen of the antifungal ketoconazole (KTZ) with primary arylsulfonamides. The aim of this study is to present the basis for a new generation of Malassezia antifungal agents able to inhibit the enzyme lanosterol-14α-demethylase (CYP51; EC 1.14.13.70) as well as a newly emergent therapeutic target: carbonic anhydrases (CAs; EC 4.2.1.1). The final compounds showed effective interactions with the intended targets in vitro, as well as KTZ comparable minimum inhibitory concentrations on yeast strains of the Malassezia genus: Malassezia furfur ATCC 14521; Malassezia globosa ATCC MYA 4612; and Malassezia pachydermatis DSM 6172. Overall, the data obtained account for the reported compounds as promising antifungal candidates with high safety profiles for the management of fungal infections.

Indexed as

14-alpha Demethylase InhibitorsAntifungal AgentsDrug DesignKetoconazoleMalasseziaDose-Response Relationship, DrugHumansMicrobial Sensitivity TestsMolecular StructureStructure-Activity Relationship14-alpha Demethylase InhibitorsAntifungal AgentsKetoconazole14α‐demethylaseantifungalscarbonic anhydrasesfungiMalassezia

Identifiers

PMID40726219
PMCPMC12304870

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.