Evidence map›Paper›PMID 22099257›Full record

ArticleBioorganic & medicinal chemistry2012

Design, synthesis, and evaluation of novel small molecule inhibitors of the influenza virus protein NS1.

Joseph J Jablonski, Dipwanita Basu, Daniel A Engel, H Mario Geysen

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.

0numbers the graph read from it
0cells of the map it votes in
26citing papers in PubMed
3.0field-weighted citation impact, top 9% 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

26 citing papers in PubMed, 40 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

4 authors at 1 institution in 1 country.

Joseph J JablonskiUniversity of Virginia, Department of Chemistry, Charlottesville, VA 22904, USA.
Dipwanita Basu
Daniel A Engel
H Mario Geysen
University of Virginia · US

Funding

Novel anti-viral agents to treat influenzaR44AI084244 · NIAID · ALEXANDER BIODISCOVERIES, LLC · PI BASU, DIPANWITA · 2013 to 2015
$3.0M
Development of Yeast-Based Assays for anti-influenza drug discoveryR01AI071341 · NIAID · UNIVERSITY OF VIRGINIA · PI ENGEL, DANIEL A · 2006 to 2006
$666k
Novel anti-viral agents to treat influenzaR43AI084244 · NIAID · ALEXANDER BIODISCOVERIES, LLC · PI BASU, DIPANWITA · 2010 to 2011
$600k
NIAID NIH HHS 5R43AI084244NIAID NIH HHS R01 AI071341NIAID NIH HHS R01AI071341NIAID NIH HHS R43 AI084244
6 · The paper itself

Abstract

Influenza is a continuing world-wide public health problem that causes significant morbidity and mortality during seasonal epidemics and sporadic pandemics. The existing vaccination program is variably effective from year to year, and drug resistance to available antivirals is a growing problem, making the development of additional antivirals an important challenge. Influenza virus non-structural protein 1 (NS1) is the centerpiece of the viral response to the host interferon (IFN) system. NS1 was demonstrated previously to be a potential therapeutic target for antiviral therapy by the identification of specific small-molecule inhibitors. One inhibitory compound, NSC125044, was subjected to chemical evaluation. Initial synthetic work comprised simplifying the core structure by removing unwanted functionality and determination of key features important for activity. Several subclasses of molecules were designed and synthesized to further probe activity and develop the basis for a structure-activity relationship. Apparent potency, as judged by activity in virus replication assays, increased dramatically for some analogs, without cytotoxicity. Results suggest that the target binding site tolerates hydrophobic bulk as well as having a preference for weakly basic substituents.

Indexed as

Drug DesignAnimalsAntiviral AgentsBenzeneCell LineDogsHydrazinesOrthomyxoviridaeSmall Molecule LibrariesViral Nonstructural Proteins2-hydroxybenzohydrazideAntiviral AgentsBenzeneHydrazinesINS1 protein, influenza virusSmall Molecule LibrariesViral Nonstructural Proteins

Identifiers

PMID22099257
PMCPMC4373408
OpenAlexW2045590420

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.