Evidence map›Paper›PMID 28682613›Full record

ArticleThe Journal of organic chemistry2017

Synthesis of a 3-Amino-2,3-dihydropyrid-4-one and Related Heterocyclic Analogues as Mechanism-Based Inhibitors of BioA, a Pyridoxal Phosphate-Dependent Enzyme.

Carter G Eiden, Courtney C Aldrich

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in The Journal of organic chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.8field-weighted citation impact, top 29% 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

4 citing papers in PubMed, 15 citations in OpenAlex.

  1. Article
  2. Review
  3. Review
  4. 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

2 authors at 1 institution in 1 country.

Carter G EidenDepartment of Medicinal Chemistry, University of Minnesota , 308 Harvard Street SE, 8-174 WDH, Minneapolis, Minnesota 55455, United States.
Courtney C AldrichDepartment of Medicinal Chemistry, University of Minnesota , 308 Harvard Street SE, 8-174 WDH, Minneapolis, Minnesota 55455, United States.ORCID 0000-0001-9261-594X
University of Minnesota · US

Funding

Chemistry-Biology Interface Training GrantT32GM008700 · NIGMS · UNIVERSITY OF MINNESOTA TWIN CITIES · PI DISTEFANO, MARK D · 1999 to 2018
$4.0M
Biotin synthesis and biotin ligation in MtbR01AI091790 · NIAID · WEILL MEDICAL COLL OF CORNELL UNIV · PI SCHNAPPINGER, DIRK · 2011 to 2015
$3.0M
NIAID NIH HHS R01 AI091790NIGMS NIH HHS T32 GM008700
6 · The paper itself

Abstract

Amiclenomycin (ACM) is a chemically unstable antibiotic with selective activity against Mycobacterium tuberculosis (Mtb) due to mechanism-based inhibition of BioA, a pyridoxal 5'-phosphate (PLP)-dependent aminotransferase. The first-generation ACM analogue dihydro-2-pyridone 1 maintains a similar bioactivation mechanism concluding with covalent labeling of the PLP cofactor. To improve on 1, we report the synthesis of dihydro-4-pyranone 2, dihydro-4-pyridone 3, and dihydro-4-thiopyranone 13, which were rationally designed to boost the rate of enzyme inactivation by lowering the pK

Indexed as

Bacterial ProteinsDose-Response Relationship, DrugEnzyme InhibitorsHeterocyclic CompoundsMolecular StructureMycobacterium tuberculosisPyridonesStructure-Activity RelationshipTransaminases3-amino-2,3-dihydropyrid-4-oneBacterial ProteinsBioA protein, bacteriaEnzyme InhibitorsHeterocyclic CompoundsPyridonesTransaminases

Identifiers

PMID28682613
PMCPMC5590672
OpenAlexW2725529302

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.