Evidence map›Paper›PMID 40712895›Full record

ArticleBioorganic & medicinal chemistry letters2025

Synthesis and evaluation of novel substituted N-(2-phenylbutyl)-5,6,7,8-tetrahydro-quinazolin-4-amines as allosteric modulators of HIV-DAT-tat interaction.

Theresa H Nguyen, Omar Moukha-Chafiq, Shuklendu Karyakarte, Ana C Jimenez-Torres, Ganesh Shrestha, Sixue Zhang, Jun Zhu, Corinne E Augelli-Szafran

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2025. 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

8 authors.

Theresa H NguyenScientific Platforms Division, Southern Research, 2000 9(th) Avenue South, Birmingham, AL 35205, USA.
Omar Moukha-ChafiqScientific Platforms Division, Southern Research, 2000 9(th) Avenue South, Birmingham, AL 35205, USA. Electronic address: omoukha-chafiq@southernresearch.org.
Shuklendu KaryakarteScientific Platforms Division, Southern Research, 2000 9(th) Avenue South, Birmingham, AL 35205, USA.
Ana C Jimenez-TorresDepartment of Drug Discovery and Biomedical Sciences, College of Pharmacy, University of South Carolina, Columbia, SC 29208, USA; Department of Pharmacology and Toxicology, Medical College of Georgia, Augusta University, Augusta, GA, 30912, USA.
Ganesh ShresthaScientific Platforms Division, Southern Research, 2000 9(th) Avenue South, Birmingham, AL 35205, USA.
Sixue ZhangScientific Platforms Division, Southern Research, 2000 9(th) Avenue South, Birmingham, AL 35205, USA.
Jun ZhuDepartment of Drug Discovery and Biomedical Sciences, College of Pharmacy, University of South Carolina, Columbia, SC 29208, USA; Department of Pharmacology and Toxicology, Medical College of Georgia, Augusta University, Augusta, GA, 30912, USA.
Corinne E Augelli-SzafranScientific Platforms Division, Southern Research, 2000 9(th) Avenue South, Birmingham, AL 35205, USA.

Funding

Molecular mechanisms: Dysregulation of monoamine transporters by HIV-1Tat and cocaineR01DA035714 · NIDA · UNIVERSITY OF SOUTH CAROLINA AT COLUMBIA · PI Jay P. McLaughlin, CHANG-GUO ZHAN · 2013 to 2026
$6.6M
Allosteric Modulators of Dopamine Transporter as Therapeutic Agents for NeuroAIDSR01DA047924 · NIDA · SOUTHERN RESEARCH INSTITUTE · PI AUGELLI-SZAFRAN, CORINNE ELIZABETH, ZHU, JUN · 2020 to 2024
$4.3M
NIDA NIH HHS R01 DA035714NIDA NIH HHS R01 DA047924
6 · The paper itself

Abstract

Allosteric modulation of interaction between Dopamine Transporter (DAT) and HIV-1 transactivator of transcription (Tat) by small molecules suggests a potential therapeutic intervention for HIV-infected patients with concurrent cocaine abuse. We have previously reported in vitro and in vivo studies on a novel allosteric modulator, SRI-32743, which was shown to attenuate Tat-induced inhibition of [

Indexed as

Dopamine Plasma Membrane Transport ProteinsHIV-1Quinazolinestat Gene Products, Human Immunodeficiency VirusAllosteric RegulationAnimalsCHO CellsCricetinaeCricetulusHumansMolecular StructureStructure-Activity RelationshipDopamine Plasma Membrane Transport ProteinsQuinazolinestat Gene Products, Human Immunodeficiency VirusDopamine uptake, dopamine transporter (DAT), HIV-1 tat proteinHIV-1 associated neurocognitive disorders (HAND)Small molecule allosteric modulators

Identifiers

PMID40712895
PMCPMC12327769

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Registered trials

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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.