Evidence map›Paper›PMID 33733986›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2021

Synthesis, biological activities and docking studies of pleuromutilin derivatives with piperazinyl urea linkage.

Yuanyuan Zhang, Chuan Xie, Yang Liu, Feng Shang, Rushiya Shao, Jing Yu, Chunxia Wu, Xinghui Yao, Dongfang Liu, Zhouyu Wang

Open access · goldAbstract read
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
3.5field-weighted citation impact, top 8% 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

7 citing papers in PubMed, 19 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

10 authors at 3 institutions in 2 countries.

Yuanyuan ZhangDepartment of Chemistry, School of Science, Xihua University, Chengdu, China.
Chuan XieDepartment of Chemistry, School of Science, Xihua University, Chengdu, China.
Yang LiuDepartment of Chemistry, School of Science, Xihua University, Chengdu, China.
Feng ShangDepartment of Chemistry, School of Science, Xihua University, Chengdu, China.
Rushiya ShaoDepartment of Chemistry, School of Science, Xihua University, Chengdu, China.
Jing YuKampo Medicine Pharmacology Research Laboratory, Graduate School of Pharmaceutical Sciences, Yokohama University of Pharmacy, Yokohama-shi, Japan.
Chunxia WuDepartment of Chemistry, School of Science, Xihua University, Chengdu, China.
Xinghui YaoDepartment of Chemistry, School of Science, Xihua University, Chengdu, China.
Dongfang LiuDepartment of Chemistry, School of Science, Xihua University, Chengdu, China.
Zhouyu WangDepartment of Chemistry, School of Science, Xihua University, Chengdu, China.
Xihua University · CNYibin University · CNYokohama University of Pharmacy · JP

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Antibiotics resistance is becoming increasingly common, involving almost all antibiotics on the market. Diseases caused by drug resistant bacteria, such as MRSA, have high mortality and negatively affect public health. The development of new drugs would be an effective means of solving this problem. Modifications based on bioactive natural products could greatly shorten drug development time and improve success rate. Pleuromutilin, a natural product from the basidiomycete bacterial species, is a promising antibiotic candidate. In this study, a series of novel pleuromutilin derivatives possessing piperazinyl urea linkage were efficiently synthesised, and their antibacterial activities and bactericidal properties were evaluated via MIC, MBC and Time-kill kinetics assays. The results showed that all compounds exhibited potent activities against tested strains, especially MRSA strains with MIC values as low as 0.125 μg/mL; 8 times lower than that of marketed antibiotic Tiamulin. Docking studies indicate substituted piperazinyl urea derivatives could provide hydrogen bonds and initiate π-π stacking between molecules and surrounding residues.

Indexed as

Molecular Docking SimulationAnti-Bacterial AgentsDiterpenesHEK293 CellsHumansMethicillin-Resistant Staphylococcus aureusMicrobial Sensitivity TestsMolecular StructurePleuromutilinsPolycyclic CompoundsUreaAnti-Bacterial AgentsDiterpenesPleuromutilinsPolycyclic CompoundsUreabiological activitiesMRSApiperazinyl ureaPleuromutilinsynthesis

Identifiers

PMID33733986
PMCPMC7993385
OpenAlexW3137769054

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.