Evidence map›Paper›PMID 31706668›Full record

ArticleBioorganic & medicinal chemistry letters2020

A new chemotype with promise against Trypanosoma cruzi.

Xiaofang Wang, Monica Cal, Marcel Kaiser, Frederick S Buckner, Galina I Lepesheva, Austin G Sanford, Alexander I Wallick, Paul H Davis, Jonathan L Vennerstrom

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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.

Xiaofang WangCollege of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, United States.
Monica CalDepartment of Medical Parasitology and Infection Biology, Swiss Tropical Institute, Socinstrasse 57, CH-4002 Basel, Switzerland; University of Basel, CH-4003 Basel, Switzerland.
Marcel KaiserDepartment of Medical Parasitology and Infection Biology, Swiss Tropical Institute, Socinstrasse 57, CH-4002 Basel, Switzerland; University of Basel, CH-4003 Basel, Switzerland.
Frederick S BucknerDepartment of Medicine, University of Washington, 750 Republican Street, Seattle, WA, United States.
Galina I LepeshevaDepartment of Biochemistry, Vanderbilt University, 2200 Pierce Ave., Nashville, TN, United States.
Austin G SanfordDepartment of Biology, University of Nebraska at Omaha, Omaha, NE, United States.
Alexander I WallickDepartment of Biology, University of Nebraska at Omaha, Omaha, NE, United States.
Paul H DavisDepartment of Biology, University of Nebraska at Omaha, Omaha, NE, United States.
Jonathan L VennerstromCollege of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, United States. Electronic address: jvenners@unmc.edu.

Funding

Structural Requirements for Sterol 14alpha-DemethylasesR01GM067871 · NIGMS · VANDERBILT UNIVERSITY · PI LEPESHEVA, GALINA I · 2004 to 2023
$7.2M
Optimization of Antischistosomal ChemotypesR01AI116723 · NIAID · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI VENNERSTROM, JONATHAN L · 2015 to 2024
$6.2M
NIAID NIH HHS R01 AI116723NIGMS NIH HHS R01 GM067871
6 · The paper itself

Abstract

Pyridyl benzamide 2 is a potent inhibitor of Trypanosoma cruzi, but not other protozoan parasites, and had a selectivity-index of ≥10. The initial structure-activity relationship (SAR) indicates that benzamide and sulfonamide functional groups, and N-methylpiperazine and sterically unhindered 3-pyridyl substructures are required for high activity against T. cruzi. Compound 2 and its active analogs had low to moderate metabolic stabilities in human and mouse liver microsomes.

Indexed as

AnimalsChagas DiseaseHumansStructure-Activity RelationshipTrypanocidal AgentsTrypanosoma cruziTrypanocidal AgentsChagas diseaseSARTrypanosoma cruzi

Identifiers

PMID31706668
PMCPMC6892603

What OpenQuestion holds

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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.