Evidence map›Paper›PMID 34156862›Full record

ArticleJournal of medicinal chemistry2021

Lead Optimization of 3,5-Disubstituted-7-Azaindoles for the Treatment of Human African Trypanosomiasis.

Dana M Klug, Eftychia M Mavrogiannaki, Katherine C Forbes, Lisseth Silva, Rosario Diaz-Gonzalez, Guiomar Pérez-Moreno, Gloria Ceballos-Pérez, Raquel Garcia-Hernández, Cristina Bosch-Navarrete, Carlos Cordón-Obras and 14 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
1.1field-weighted citation impact, top 23% of its field
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

6 citing papers in PubMed, 10 citations in OpenAlex.

  1. Review
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  3. AI-DrivenJournal of medicinal chemistry · 2025
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  6. 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

24 authors at 4 institutions in 2 countries.

Dana M KlugDepartment of Chemistry & Chemical Biology, Northeastern University, 360 Huntington Avenue, Boston, Massachusetts 02115, United States.ORCID 0000-0002-8982-0640
Eftychia M MavrogiannakiDepartment of Chemistry & Chemical Biology, Northeastern University, 360 Huntington Avenue, Boston, Massachusetts 02115, United States.
Katherine C ForbesDepartment of Chemistry & Chemical Biology, Northeastern University, 360 Huntington Avenue, Boston, Massachusetts 02115, United States.
Lisseth SilvaDepartment of Chemistry & Chemical Biology, Northeastern University, 360 Huntington Avenue, Boston, Massachusetts 02115, United States.
Rosario Diaz-GonzalezInstituto de Parasitología y Biomedicina "López-Neyra" Consejo Superior de Investigaciones Científicas (CSIC), Granada 18016, Spain.
Guiomar Pérez-MorenoInstituto de Parasitología y Biomedicina "López-Neyra" Consejo Superior de Investigaciones Científicas (CSIC), Granada 18016, Spain.
Gloria Ceballos-PérezInstituto de Parasitología y Biomedicina "López-Neyra" Consejo Superior de Investigaciones Científicas (CSIC), Granada 18016, Spain.
Raquel Garcia-HernándezInstituto de Parasitología y Biomedicina "López-Neyra" Consejo Superior de Investigaciones Científicas (CSIC), Granada 18016, Spain.
Cristina Bosch-NavarreteInstituto de Parasitología y Biomedicina "López-Neyra" Consejo Superior de Investigaciones Científicas (CSIC), Granada 18016, Spain.
Carlos Cordón-ObrasInstituto de Parasitología y Biomedicina "López-Neyra" Consejo Superior de Investigaciones Científicas (CSIC), Granada 18016, Spain.
Claudia Gómez-LiñánInstituto de Parasitología y Biomedicina "López-Neyra" Consejo Superior de Investigaciones Científicas (CSIC), Granada 18016, Spain.
Andreu SauraInstituto de Parasitología y Biomedicina "López-Neyra" Consejo Superior de Investigaciones Científicas (CSIC), Granada 18016, Spain.
Jeremiah D MomperCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, 9500 Gilman Drive, La Jolla, San Diego, California 92093, United States.
Maria Santos Martinez-MartinezDiseases of the Developing World (DDW), Tres Cantos Medicines Development Campus, GlaxoSmithKline, Tres Cantos 28760, Spain.
Pilar ManzanoDiseases of the Developing World (DDW), Tres Cantos Medicines Development Campus, GlaxoSmithKline, Tres Cantos 28760, Spain.
Ali SyedCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, 9500 Gilman Drive, La Jolla, San Diego, California 92093, United States.
Nelly El-SakkaryCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, 9500 Gilman Drive, La Jolla, San Diego, California 92093, United States.
Conor R CaffreyCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, 9500 Gilman Drive, La Jolla, San Diego, California 92093, United States.
Francisco GamarroInstituto de Parasitología y Biomedicina "López-Neyra" Consejo Superior de Investigaciones Científicas (CSIC), Granada 18016, Spain.
Luis Miguel Ruiz-PerezInstituto de Parasitología y Biomedicina "López-Neyra" Consejo Superior de Investigaciones Científicas (CSIC), Granada 18016, Spain.
Dolores Gonzalez PacanowskaInstituto de Parasitología y Biomedicina "López-Neyra" Consejo Superior de Investigaciones Científicas (CSIC), Granada 18016, Spain.ORCID 0000-0002-4303-5209
Lori FerrinsDepartment of Chemistry & Chemical Biology, Northeastern University, 360 Huntington Avenue, Boston, Massachusetts 02115, United States.ORCID 0000-0001-8992-0919
Miguel NavarroInstituto de Parasitología y Biomedicina "López-Neyra" Consejo Superior de Investigaciones Científicas (CSIC), Granada 18016, Spain.
Michael P PollastriDepartment of Chemistry & Chemical Biology, Northeastern University, 360 Huntington Avenue, Boston, Massachusetts 02115, United States.ORCID 0000-0001-9943-7197
Consejo Superior de Investigaciones Científicas · ESNortheastern University · USCenter for Discovery · USGlaxoSmithKline (Spain) · ES

Funding

Optimization and Modes of Action of NEU-4438, a New Anti-trypanosome Lead DrugR01AI124046 · NIAID · NORTHEASTERN UNIVERSITY · PI FERRINS, LORI, MENSA-WILMOT, KOJO A. · 2016 to 2025
$6.0M
Repurposing human kinase inhibitor chemotypes for Neglected Tropical DiseasesR01AI114685 · NIAID · NORTHEASTERN UNIVERSITY · PI FERRINS, LORI · 2015 to 2025
$4.6M
Lead optimization of agents targeting multiple kinetoplastid parasitesR21AI127594 · NIAID · NORTHEASTERN UNIVERSITY · PI POLLASTRI, MICHAEL P · 2017 to 2018
$427k
Defining the death transcriptome of Schistosoma mansoni to construct a molecular drug screenR21AI126296 · NIAID · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI CAFFREY, CONOR · 2017 to 2018
$415k
NIAID NIH HHS R01 AI114685NIAID NIH HHS R01 AI124046NIAID NIH HHS R21 AI126296NIAID NIH HHS R21 AI127594
6 · The paper itself

Abstract

Neglected tropical diseases such as human African trypanosomiasis (HAT) are prevalent primarily in tropical climates and among populations living in poverty. Historically, the lack of economic incentive to develop new treatments for these diseases has meant that existing therapeutics have serious shortcomings in terms of safety, efficacy, and administration, and better therapeutics are needed. We now report a series of 3,5-disubstituted-7-azaindoles identified as growth inhibitors of

Indexed as

Dose-Response Relationship, DrugHumansIndolesMolecular StructureParasitic Sensitivity TestsStructure-Activity RelationshipTrypanocidal AgentsTrypanosoma brucei bruceiTrypanosomiasis, African7-azaindole dimerIndolesTrypanocidal Agents

Identifiers

PMID34156862
PMCPMC8412142
OpenAlexW3176321212

What OpenQuestion holds

Textmetadata
LicenceTDM
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.