Evidence map›Paper›PMID 35450361›Full record

ArticleACS medicinal chemistry letters2022

Development of 6-Methanesulfonyl-8-nitrobenzothiazinone Based Antitubercular Agents.

Rui Shi, Bin Wang, Giovanni Stelitano, Xiaomei Wu, Yuanyuan Shan, Yue Wu, Xin Wang, Laurent R Chiarelli, Yu Lu, Chunhua Qiao

Abstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing 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

3 citing papers in PubMed.

  1. Review
  2. Article
  3. 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

10 authors.

Rui ShiCollege of Pharmaceutical Sciences, Soochow University, 199 Renai Road, Suzhou 215123, P. R. China.
Bin WangBeijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research, Beijing Chest Hospital, 97 Ma Chang Street, Beijing 101149, P. R. China.
Giovanni StelitanoDepartment of Biology and Biotechnology, University of Pavia, Via Ferrata 9, 27100 Pavia, Italy.ORCID https://orcid.org/0000-0002-5219-4770
Xiaomei WuCollege of Pharmaceutical Sciences, Soochow University, 199 Renai Road, Suzhou 215123, P. R. China.
Yuanyuan ShanCollege of Pharmaceutical Sciences, Soochow University, 199 Renai Road, Suzhou 215123, P. R. China.
Yue WuCollege of Pharmaceutical Sciences, Soochow University, 199 Renai Road, Suzhou 215123, P. R. China.
Xin WangCollege of Pharmaceutical Sciences, Soochow University, 199 Renai Road, Suzhou 215123, P. R. China.
Laurent R ChiarelliDepartment of Biology and Biotechnology, University of Pavia, Via Ferrata 9, 27100 Pavia, Italy.ORCID https://orcid.org/0000-0003-0348-9764
Yu LuBeijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research, Beijing Chest Hospital, 97 Ma Chang Street, Beijing 101149, P. R. China.
Chunhua QiaoCollege of Pharmaceutical Sciences, Soochow University, 199 Renai Road, Suzhou 215123, P. R. China.ORCID https://orcid.org/0000-0002-7736-449X

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The 6-trifluoro substituted 8-nitrobenzothiazinones (BTZs) represent a novel type of antitubercular agents, and their high antimycobacterial activity is related to the inhibition of decaprenylphosphoryl-β-d-ribose 2'-oxidase (DprE1), an enzyme essential for the biosynthesis of mycobacterial cell wall. While extraordinary whole-cell activity was reported for the clinically advanced compound PBTZ169, its poor aqueous solubility signals the potential low bioavailability. To ameliorate the BTZ physiochemical property, a series of 6-methanesulfonyl substituted compounds were designed and prepared, and their antitubercular activity and DprE1 inhibition ability were evaluated. Among these compounds, MsPBTZ169 and compounds

Identifiers

PMID35450361
PMCPMC9014434

What OpenQuestion holds

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Registered trials

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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.