Evidence map›Paper›PMID 28536876›Full record

ArticleMolecular diversity2017

Design and one-pot synthesis of 2-thiazolylhydrazone derivatives as influenza neuraminidase inhibitors.

Keyang Yuan, Mengwu Xiao, Ying Tan, Jiao Ye, Yongle Xie, Xiaoxiao Sun, Aixi Hu, Wenwen Lian, Ailin Liu

Abstract read
PubMed Publisher
In one paragraph

Article in Molecular diversity, 2017. 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

9 authors.

Keyang YuanCollege of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, China.
Mengwu XiaoCollege of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, China.
Ying TanCollege of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, China.
Jiao YeCollege of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, China. yejiao@hnu.edu.cn.ORCID http://orcid.org/0000-0002-9725-0553
Yongle XieCollege of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, China.
Xiaoxiao SunCollege of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, China.
Aixi HuCollege of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, China. axhu@hnu.edu.cn.
Wenwen LianInstitute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China.
Ailin LiuInstitute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China.

Funding

Emergency Project of National Natural Science Fund No. 21442014
6 · The paper itself

Abstract

Two series of novel 2-thiazolylhydrazone derivatives were designed and synthesized via one-pot reaction of benzaldehyde derivatives, [Formula: see text]-haloketones and thiosemicarbazide. The structures of compounds 1 and 2 were characterized by [Formula: see text] NMR and [Formula: see text] NMR, and compound 1g was further confirmed by X-ray crystallography. All of the target compounds were evaluated for their NA inhibitory activity against influenza viral neuraminidase (H1N1) in vitro, and the results showed that many compounds exhibited moderate to strong inhibitory activities against influenza viral neuraminidase (H1N1). Among them, compounds 1p, 1q and 2c showed the most potent inhibitory activities with [Formula: see text] values ranging from 10.50 to [Formula: see text]. Our structure-activity relationship analysis indicated that 2-thiazolylhydrazone is an effective scaffold for NA inhibitors and that introducing an ethoxycarbonyl group to the 5-position of thiazole ring could enhance inhibitory potency. Molecular docking was performed on the most active compounds 1p and 2c to provide more insight into their mechanism of interaction.

Indexed as

Antiviral AgentsCrystallography, X-RayDrug DesignEnzyme InhibitorsHydrazonesInfluenza A Virus, H1N1 SubtypeInhibitory Concentration 50Molecular Docking SimulationMolecular StructureNeuraminidaseStructure-Activity RelationshipThiazolesAntiviral AgentsEnzyme InhibitorsHydrazonesNeuraminidaseThiazolesMolecular dockingNeuraminidase (NA) inhibitorsOne-pot reactionThiazolylhydrazones

Identifiers

PMID28536876

What OpenQuestion holds

Textmetadata
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.