Evidence map›Paper›PMID 40504040›Full record

ArticleChemMedChem2025

Antiprotozoal Activity of Highly Substituted Pyrazole and Pyrimidine Derivatives.

Matteo Lusardi, Nicoletta Basilico, Erika Iervasi, Chiara Brullo, Silvia Parapini, Marco Ponassi, Camillo Rosano, Andrea Spallarossa

Abstract read
In one paragraph

Article in ChemMedChem, 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. Article
  2. Review
  3. 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

8 authors.

Matteo LusardiDepartment of Pharmacy, Università degli Studi di Genova, viale Benedetto XV, 3, 16132, Genova, Italy.ORCID https://orcid.org/0000-0002-7003-7891
Nicoletta BasilicoDipartimento di Scienze Biomediche, Chirurgiche e Odontoiatriche, Università degli Studi di Milano, Via della Commenda, 10, 20133, Milan, Italy.ORCID https://orcid.org/0000-0001-9030-1066
Erika IervasiProteomics and Mass Spectrometry Unit, IRCCS Ospedale Policlinico San Martino, L.go R. Benzi, 10, 16132, Genova, Italy.ORCID https://orcid.org/0000-0002-7531-3373
Chiara BrulloDepartment of Pharmacy, Università degli Studi di Genova, viale Benedetto XV, 3, 16132, Genova, Italy.ORCID https://orcid.org/0000-0002-2575-7726
Silvia ParapiniDipartimento di Scienze Biomediche per la Salute, Università degli Studi di Milano, Via Pascal, 36, 20133, Milan, Italy.ORCID https://orcid.org/0000-0003-2079-8892
Marco PonassiProteomics and Mass Spectrometry Unit, IRCCS Ospedale Policlinico San Martino, L.go R. Benzi, 10, 16132, Genova, Italy.ORCID https://orcid.org/0000-0002-5418-2458
Camillo RosanoProteomics and Mass Spectrometry Unit, IRCCS Ospedale Policlinico San Martino, L.go R. Benzi, 10, 16132, Genova, Italy.ORCID https://orcid.org/0000-0003-2949-9215
Andrea SpallarossaDepartment of Pharmacy, Università degli Studi di Genova, viale Benedetto XV, 3, 16132, Genova, Italy.ORCID https://orcid.org/0000-0002-3360-7146

Funding

Italian Ministry of HealthUniversità degli Studi di Genova
6 · The paper itself

Abstract

To further extend the structure-activity relationships of previously reported antimalarial anilino-pyrazoles VI, trisubstituted pyrazoles 13-15, and pyrimidines 16 and 17 are designed and synthesized. The novel derivatives are prepared thorough a divergent, chemo-selective approach starting from N,S-acetal intermediates. Compounds 13-17 are tested for their antimalarial and antileishmanial activity and their cytotoxicity is evaluated against human fibroblast. Pyrazoles 14 d,e and pyrimidine 17e are identified as novel and effective antiplasmodial agents being able to inhibit, at micromolar concentrations, chloroquine(CQ)-sensitive and CQ-resistant Plasmodium falciparum strains, as well as Leishmania infatum and Leishmania tropica protozoa. Additionally, favorable pharmacokinetics and toxicity profiles are predicted for the compounds.

Indexed as

Antiprotozoal AgentsPyrazolesPyrimidinesHumansLeishmaniaLeishmania tropicaParasitic Sensitivity TestsPlasmodium falciparumStructure-Activity RelationshipAntiprotozoal AgentsPyrazolesPyrimidinesantileishmanial agentsantimalarial agentspyrazole compoundspyrimidine derivatives

Identifiers

PMID40504040
PMCPMC12368482

What Socratic 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 Socratic graph.