Evidence map›Paper›PMID 24614386›Full record

ArticleAntimicrobial agents and chemotherapy2014

2-Aminothiazolones as anti-HIV agents that act as gp120-CD4 inhibitors.

Marika Tiberi, Cristina Tintori, Elisa Rita Ceresola, Roberta Fazi, Claudio Zamperini, Pierpaolo Calandro, Luigi Franchi, Manikandan Selvaraj, Lorenzo Botta, Michela Sampaolo and 5 more

Open access · bronzeAbstract read
In one paragraph

Article in Antimicrobial agents and chemotherapy, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.9field-weighted citation impact, top 27% 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

5 citing papers in PubMed, 13 citations in OpenAlex.

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  5. 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

15 authors at 4 institutions in 2 countries.

Marika TiberiDipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Siena, Italy.
Cristina TintoriDipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Siena, Italy.
Elisa Rita CeresolaUniversity Vita-Salute San Raffaele, Milan, Italy.
Roberta FaziDipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Siena, Italy.
Claudio ZamperiniDipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Siena, Italy.
Pierpaolo CalandroDipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Siena, Italy.
Luigi FranchiDipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Siena, Italy.
Manikandan SelvarajDipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Siena, Italy.
Lorenzo BottaDipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Siena, Italy.
Michela SampaoloUniversity Vita-Salute San Raffaele, Milan, Italy Ospedale San Raffale, Milan, Italy.
Diego SaitaUniversity Vita-Salute San Raffaele, Milan, Italy Ospedale San Raffale, Milan, Italy.
Roberto FerrareseOspedale San Raffale, Milan, Italy.
Massimo ClementiUniversity Vita-Salute San Raffaele, Milan, Italy Ospedale San Raffale, Milan, Italy.
Filippo CanducciOspedale San Raffale, Milan, Italy Department of Clinical and Experimental Medicine, Università degli Studi dell'Insubria, Varese, Italy canducci.filippo@hsr.it botta.maurizio@gmail.com.
Maurizio BottaDipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Siena, Italy Biotechnology College of Science and Technology, Temple University, Biolife Science Building, Philadelphia, Pennsylvania, USA canducci.filippo@hsr.it botta.maurizio@gmail.com.
University of Siena · ITIRCCS Ospedale San Raffaele · ITUniversity of Insubria · ITVita-Salute San Raffaele University · IT

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

We report here the synthesis of 2-aminothiazolones along with their biological properties as novel anti-HIV agents. Such compounds have proven to act through the inhibition of the gp120-CD4 protein-protein interaction that occurs at the very early stage of the HIV-1 entry process. No cytotoxicity was found for these compounds, and broad antiviral activities against laboratory strains and pseudotyped viruses were documented. Docking simulations have also been applied to predict the mechanism, at the molecular level, by which the inhibitors were able to interact within the Phe43 cavity of HIV-1 gp120. Furthermore, a preliminary absorption, distribution, metabolism, and excretion (ADME) evaluation was performed. Overall, this study led the basis for the development of more potent HIV entry inhibitors.

Indexed as

Anti-HIV AgentsCD4 AntigensCell LineHIV-1HIV Envelope Protein gp120HIV Fusion InhibitorsHumansMolecular Docking SimulationProtein BindingAnti-HIV AgentsCD4 AntigensHIV Envelope Protein gp120HIV Fusion Inhibitors

Identifiers

PMID24614386
PMCPMC4068444
OpenAlexW2115113205

What OpenQuestion holds

Textmetadata
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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.