Evidence map›Paper›PMID 22639134›Full record

ArticleChemMedChem2012

Selectively guanidinylated aminoglycosides as antibiotics.

Richard J Fair, Mary E Hensler, Wdee Thienphrapa, Quang N Dam, Victor Nizet, Yitzhak Tor

Open access · greenAbstract read
In one paragraph

Article in ChemMedChem, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.

0numbers the graph read from it
0cells of the map it votes in
23citing papers in PubMed
3.4field-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

23 citing papers in PubMed, 47 citations in OpenAlex.

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  16. Tobramycin Variants with Enhanced Ribosome-Targeting Activity.Chembiochem : a European journal of chemical biology · 2015
    Article
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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

6 authors at 1 institution in 1 country.

Richard J FairDepartment of Chemistry & Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA.
Mary E Hensler
Wdee Thienphrapa
Quang N Dam
Victor Nizet
Yitzhak Tor
University of California, San Diego · US

Funding

Fluorescent Nucleosides and OligonucleotidesR01GM069773 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI TOR, YITZHAK · 2004 to 2020
$5.0M
TRAINING & OUTREACH COREU54HD071600 · NICHD · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI CAPPARELLI, EDMUND VINCENT · 2011 to 2015
$3.6M
NICHD NIH HHS HD071600NICHD NIH HHS U54 HD071600NIGMS NIH HHS GM069773NIGMS NIH HHS R01 GM069773
6 · The paper itself

Abstract

The emergence of virulent, drug-resistant bacterial strains coupled with a minimal output of new pharmaceutical agents to combat them makes this a critical time for antibacterial research. Aminoglycosides are a well-studied, highly potent class of naturally occurring antibiotics with scaffolds amenable to modification, and therefore, they provide an excellent starting point for the development of semisynthetic, next-generation compounds. To explore the potential of this approach, we synthesized a small library of aminoglycoside derivatives selectively and minimally modified at one or two positions with a guanidine group replacing the corresponding amine or hydroxy functionality. Most guanidino-aminoglycosides showed increased affinity for the ribosomal decoding rRNA site, the cognate biological target of the natural products, when compared with their parent antibiotics, as measured by an in vitro fluorescence resonance energy transfer (FRET) A-site binding assay. Additionally, certain analogues showed improved minimum inhibitory concentration (MIC) values against resistant bacterial strains, including methicillin-resistant Staphylococcus aureus (MRSA). An amikacin derivative holds particular promise with activity greater than or equal to the parent antibiotic in the majority of bacterial strains tested.

Indexed as

AminoglycosidesAnti-Bacterial AgentsBacteriaDose-Response Relationship, DrugDrug DesignGuanidinesMicrobial Sensitivity TestsMolecular ConformationStereoisomerismStructure-Activity RelationshipAminoglycosidesAnti-Bacterial AgentsGuanidines

Identifiers

PMID22639134
PMCPMC3383777
OpenAlexW1969383148

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.