Evidence map›Paper›PMID 36235118›Full record

ArticleMolecules (Basel, Switzerland)2022

Preliminary Structure-Activity Relationship Study of the MMV Pathogen Box Compound MMV675968 (2,4-Diaminoquinazoline) Unveils Novel Inhibitors of

Darline Dize, Rolland Bantar Tata, Rodrigue Keumoe, Rufin Marie Kouipou Toghueo, Mariscal Brice Tchatat, Cyrille Ngansop Njanpa, Vianey Claire Tchuenguia, Lauve Tchokouaha Yamthe, Patrick Valere Tsouh Fokou, Benoît Laleu and 3 more

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
1.7field-weighted citation impact, top 15% 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

7 citing papers in PubMed, 11 citations in OpenAlex.

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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

13 authors at 3 institutions in 3 countries.

Darline DizeAntimicrobial and Biocontrol Agents Unit (AmBcAU), Laboratory for Phytobiochemistry and Medicinal Plants Studies, Department of Biochemistry, Faculty of Science, University of Yaoundé I, Yaoundé P.O. Box 812, Cameroon.
Rolland Bantar TataResearch Unit in Bioinformatics (RUBi), Department of Biochemistry and Microbiology, Rhodes University, Grahamstown 6139, South Africa.ORCID 0000-0002-8814-5241
Rodrigue KeumoeAntimicrobial and Biocontrol Agents Unit (AmBcAU), Laboratory for Phytobiochemistry and Medicinal Plants Studies, Department of Biochemistry, Faculty of Science, University of Yaoundé I, Yaoundé P.O. Box 812, Cameroon.
Rufin Marie Kouipou ToghueoAntimicrobial and Biocontrol Agents Unit (AmBcAU), Laboratory for Phytobiochemistry and Medicinal Plants Studies, Department of Biochemistry, Faculty of Science, University of Yaoundé I, Yaoundé P.O. Box 812, Cameroon.ORCID 0000-0003-2144-0710
Mariscal Brice TchatatAntimicrobial and Biocontrol Agents Unit (AmBcAU), Laboratory for Phytobiochemistry and Medicinal Plants Studies, Department of Biochemistry, Faculty of Science, University of Yaoundé I, Yaoundé P.O. Box 812, Cameroon.
Cyrille Ngansop NjanpaAntimicrobial and Biocontrol Agents Unit (AmBcAU), Laboratory for Phytobiochemistry and Medicinal Plants Studies, Department of Biochemistry, Faculty of Science, University of Yaoundé I, Yaoundé P.O. Box 812, Cameroon.
Vianey Claire TchuenguiaAntimicrobial and Biocontrol Agents Unit (AmBcAU), Laboratory for Phytobiochemistry and Medicinal Plants Studies, Department of Biochemistry, Faculty of Science, University of Yaoundé I, Yaoundé P.O. Box 812, Cameroon.
Lauve Tchokouaha YamtheAntimicrobial and Biocontrol Agents Unit (AmBcAU), Laboratory for Phytobiochemistry and Medicinal Plants Studies, Department of Biochemistry, Faculty of Science, University of Yaoundé I, Yaoundé P.O. Box 812, Cameroon.
Patrick Valere Tsouh FokouAntimicrobial and Biocontrol Agents Unit (AmBcAU), Laboratory for Phytobiochemistry and Medicinal Plants Studies, Department of Biochemistry, Faculty of Science, University of Yaoundé I, Yaoundé P.O. Box 812, Cameroon.ORCID 0000-0003-3724-3527
Benoît LaleuMedicines for Malaria Venture, Route de Pré-Bois 20, 1215 Meyrin, Switzerland.ORCID 0000-0002-7530-2113
James DuffyMedicines for Malaria Venture, Route de Pré-Bois 20, 1215 Meyrin, Switzerland.
Ozlem Tastan BishopResearch Unit in Bioinformatics (RUBi), Department of Biochemistry and Microbiology, Rhodes University, Grahamstown 6139, South Africa.ORCID 0000-0001-6861-7849
Fabrice Fekam BoyomAntimicrobial and Biocontrol Agents Unit (AmBcAU), Laboratory for Phytobiochemistry and Medicinal Plants Studies, Department of Biochemistry, Faculty of Science, University of Yaoundé I, Yaoundé P.O. Box 812, Cameroon.ORCID 0000-0002-3147-364X
Université de Yaoundé I · CMMedicines for Malaria Venture · CHRhodes University · ZA

Funding

AAS- Grand Challenges Africa GCA/DD/rnd3/006
6 · The paper itself

Abstract

New drugs are urgently needed for the treatment of human African trypanosomiasis (HAT). In line with our quest for novel inhibitors of trypanosomes, a small library of analogs of the antitrypanosomal hit (MMV675968) available at MMV as solid materials was screened for antitrypanosomal activity. In silico exploration of two potent antitrypanosomal structural analogs (

Indexed as

Trypanocidal AgentsTrypanosomaTrypanosoma brucei bruceiTrypanosomiasis, AfricanAnimalsHumansIronLigandsQuinazolinesStructure-Activity RelationshipTetrahydrofolate Dehydrogenase2,4-diaminoquinazolineIronLigandsQuinazolinesTetrahydrofolate DehydrogenaseTrypanocidal AgentsantitrypanosomalDHFR inhibitorDNA fragmentationin silicoMMV675968 (2,4-diaminoquinazoline)MMV Pathogen Boxstructure–activity relationshiptime-kill kineticTrypanosoma brucei brucei

Identifiers

PMID36235118
PMCPMC9571290
OpenAlexW4303959045

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.