Evidence map›Paper›PMID 23009169›Full record

ArticleJournal of medicinal chemistry2012

Development of oseltamivir phosphonate congeners as anti-influenza agents.

Ting-Jen R Cheng, Steven Weinheimer, E Bart Tarbet, Jia-Tsrong Jan, Yih-Shyun E Cheng, Jiun-Jie Shie, Chun-Lin Chen, Chih-An Chen, Wei-Che Hsieh, Pei-Wei Huang and 5 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2012. 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
3.1field-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

6 citing papers in PubMed, 50 citations in OpenAlex.

  1. Article
  2. Review
  3. Synthesis and Biological Evaluation ofMolecules (Basel, Switzerland) · 2019
    Article
  4. Article
  5. Review
  6. Article
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 5 institutions in 2 countries.

Ting-Jen R ChengThe Genomics Research Center, Academia Sinica , No. 128, Sec. 2, Academia Road, Taipei 11529, Taiwan.
Steven Weinheimer
E Bart Tarbet
Jia-Tsrong Jan
Yih-Shyun E Cheng
Jiun-Jie Shie
Chun-Lin Chen
Chih-An Chen
Wei-Che Hsieh
Pei-Wei Huang
Wen-Hao Lin
Shi-Yun Wang
Jim-Min Fang
Oliver Yoa-Pu Hu
Chi-Huey Wong
Genomics Research Center, Academia Sinica · TWNational Taiwan University · TWNational Defense Medical Center · TWBiolog (United States) · USUtah State University · US

Funding

T CELL MEMORY TO VIRUSESR01AI030048 · NIAID · UNIVERSITY OF CALIFORNIA LOS ANGELES · PI AHMED, RAFI · 1990 to 2022
$5.2M
T CELL MEMORY TO VIRUSESR37AI030048 · NIAID · EMORY UNIVERSITY · PI AHMED, RAFI · 2001 to 2010
$3.9M
MACROPHAGE DEFENSES AGAINST HAEMOPHILUS INFLUENZAER29AI030063 · NIAID · WEILL MEDICAL COLLEGE OF CORNELL UNIV · PI NOEL, GARY J. · 1990 to 1994
–
NIAID NIH HHS N01 AI030048NIAID NIH HHS N01 AI030063
6 · The paper itself

Abstract

Oseltamivir phosphonic acid (tamiphosphor, 3a), its monoethyl ester (3c), guanidino-tamiphosphor (4a), and its monoethyl ester (4c) are potent inhibitors of influenza neuraminidases. They inhibit the replication of influenza viruses, including the oseltamivir-resistant H275Y strain, at low nanomolar to picomolar levels, and significantly protect mice from infection with lethal doses of influenza viruses when orally administered with 1 mg/kg or higher doses. These compounds are stable in simulated gastric fluid, liver microsomes, and human blood and are largely free from binding to plasma proteins. Pharmacokinetic properties of these inhibitors are thoroughly studied in dogs, rats, and mice. The absolute oral bioavailability of these compounds was lower than 12%. No conversion of monoester 4c to phosphonic acid 4a was observed in rats after intravenous administration, but partial conversion of 4c was observed with oral administration. Advanced formulation may be investigated to develop these new anti-influenza agents for better therapeutic use.

Indexed as

AcetamidesAdministration, OralAlphainfluenzavirusAnimalsAntiviral AgentsBetainfluenzavirusBiological AvailabilityBlood ProteinsCyclohexenesCytopathogenic Effect, ViralDogsDrug Resistance, ViralDrug StabilityFemaleHumansInfluenza A Virus, H1N1 SubtypeAcetamidesAntiviral AgentsBlood ProteinsCyclohexenesNeuraminidaseOseltamivirPhosphorous Acidstamiphosphor

Identifiers

PMID23009169
PMCPMC3492761
OpenAlexW2103490906

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.