Evidence map›Paper›PMID 35091169›Full record

ArticleBioorganic & medicinal chemistry2022

Structure-activity and structure-property relationship studies of spirocyclic chromanes with antimalarial activity.

Iredia D Iyamu, Yingzhao Zhao, Prakash T Parvatkar, Bracken F Roberts, Debora R Casandra, Lukasz Wojtas, Dennis E Kyle, Debopam Chakrabarti, Roman Manetsch

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. 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

9 authors.

Iredia D IyamuDepartment of Chemistry and Chemical Biology, College of Science, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, USA.
Yingzhao ZhaoDepartment of Chemistry and Chemical Biology, College of Science, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, USA.
Prakash T ParvatkarDepartment of Chemistry and Chemical Biology, College of Science, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, USA.
Bracken F RobertsMolecular Microbiology Division, Burnett School of Biomedical Science, University of Central Florida, 12722 Research Parkway, Orlando, FL 32826, USA.
Debora R CasandraDepartment of Global Health, College of Public Health, University of South Florida, 3720 Spectrum Boulevard, Tampa, FL 33612, USA.
Lukasz WojtasDepartment of Chemistry, University of South Florida, 4202 E. Fowler Ave, Tampa, FL 33620, USA.
Dennis E KyleDepartment of Global Health, College of Public Health, University of South Florida, 3720 Spectrum Boulevard, Tampa, FL 33612, USA; Center for Tropical and Emerging Global Diseases, University of Georgia, Athens, 500 D.W. Brooks Dr, Athens, GA 30602, USA.
Debopam ChakrabartiMolecular Microbiology Division, Burnett School of Biomedical Science, University of Central Florida, 12722 Research Parkway, Orlando, FL 32826, USA.
Roman ManetschDepartment of Chemistry and Chemical Biology, College of Science, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, USA; Department of Pharmaceutical Sciences, Bouvé College of Pharmacy, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, USA; Center for Drug Discovery, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, USA.

Funding

Orally Bioavailable 4(1H)-Quinolones with Multi-Stage Antimalarial ActivityR01AI144464 · NIAID · NORTHEASTERN UNIVERSITY · PI KYLE, DENNIS E, MANETSCH, ROMAN · 2019 to 2023
$3.6M
Natural Product-Inspired Novel Synthetic Antiplasmodial ScaffoldsR03AI117298 · NIAID · UNIVERSITY OF CENTRAL FLORIDA · PI CHAKRABARTI, DEBOPAM · 2015 to 2016
$144k
NIAID NIH HHS R01 AI144464NIAID NIH HHS R03 AI117298
6 · The paper itself

Abstract

Malaria is a prevalent and lethal disease. The fast emergence and spread of resistance to current therapies is a major concern and the development of a novel line of therapy that could overcome, the problem of drug resistance, is imperative. Screening of a set of compounds with drug/natural product-based sub-structural motifs led to the identification of spirocyclic chroman-4-one 1 with promising antimalarial activity against the chloroquine-resistant Dd2 and chloroquine-sensitive 3D7 strains of the parasite. Extensive structure-activity and structure-property relationship studies were conducted to identify the essential features necessary for its activity and properties.

Indexed as

AntimalarialsCell SurvivalChromansCrystallography, X-RayDose-Response Relationship, DrugHep G2 CellsHumansMalariaModels, MolecularMolecular StructureParasitic Sensitivity TestsPlasmodiumSpiro CompoundsStructure-Activity RelationshipAntimalarialsChromansSpiro CompoundsAntimalarialDrug resistanceNatural productsSpirocyclic chromaneStructure-activity relationshipStructure-property relationship

Identifiers

PMID35091169
PMCPMC9233738

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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.