Evidence map›Paper›PMID 29727185›Full record

ArticleJournal of medicinal chemistry2018

Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria.

Aleksey I Gerasyuto, Michael A Arnold, Jiashi Wang, Guangming Chen, Xiaoyan Zhang, Sean Smith, Matthew G Woll, John Baird, Nanjing Zhang, Neil G Almstead and 8 more

Erratum issuedOpen access · hybridAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.8field-weighted citation impact, top 28% 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

5 citing papers in PubMed, 18 citations in OpenAlex.

  1. Lactam Framework Editing via Formal Methylene Deletion.Journal of the American Chemical Society · 2026
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4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

18 authors at 1 institution in 1 country.

Aleksey I GerasyutoPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
Michael A ArnoldPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.ORCID 0000-0002-2560-9360
Jiashi WangPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
Guangming ChenPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
Xiaoyan ZhangPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
Sean SmithPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
Matthew G WollPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
John BairdPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
Nanjing ZhangPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
Neil G AlmsteadPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
Jana NarasimhanPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
Srinivasa PeddiPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
Melissa DumblePTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
Josephine SheedyPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
Marla WeetallPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
Arthur A BranstromPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
J V N PrasadPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
Gary M KarpPTC Therapeutics, Inc. , 100 Corporate Court , South Plainfield , New Jersey 07080 , United States.
PTC Therapeutics (United States) · US

Funding

Wellcome Trust
6 · The paper itself

Abstract

There exists an urgent medical need to identify new chemical entities (NCEs) targeting multidrug resistant (MDR) bacterial infections, particularly those caused by Gram-negative pathogens. 4-Hydroxy-2-pyridones represent a novel class of nonfluoroquinolone inhibitors of bacterial type II topoisomerases active against MDR Gram-negative bacteria. Herein, we report on the discovery and structure-activity relationships of a series of fused indolyl-containing 4-hydroxy-2-pyridones with improved in vitro antibacterial activity against fluoroquinolone resistant strains. Compounds 6o and 6v are representative of this class, targeting both bacterial DNA gyrase and topoisomerase IV (Topo IV). In an abbreviated susceptibility screen, compounds 6o and 6v showed improved MIC

Indexed as

Drug DiscoveryAnimalsAnti-Bacterial AgentsDNA Topoisomerases, Type IIDrug Resistance, Multiple, BacterialFemaleGram-Negative BacteriaMiceMicrobial Sensitivity TestsModels, MolecularMolecular StructureProtein ConformationPyridinesSepsisStructure-Activity RelationshipTopoisomerase II InhibitorsAnti-Bacterial AgentsDNA Topoisomerases, Type IIPyridinesTopoisomerase II Inhibitors

Identifiers

PMID29727185
PMCPMC5991783
OpenAlexW2801131812

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.