Evidence map›Paper›PMID 36312355›Full record

ArticleACS omega2022

Synthesis and Characterization of Functionalized Amino Dihydropyrimidines Toward the Analysis of their Antibacterial Structure-Activity Relationships and Mechanism of Action.

Zachary W Boyer, Hannah Kessler, Hannah Brosman, Kirsten J Ruud, Alan F Falkowski, Constance Viollet, Christina R Bourne, Matthew C O'Reilly

Open access · goldAbstract read
In one paragraph

Article in ACS omega, 2022. 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
1.3field-weighted citation impact, top 22% 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, 13 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. Review
  5. Article
  6. Article
  7. Article
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

8 authors at 3 institutions in 1 country.

Zachary W BoyerDepartment of Chemistry, Villanova University, Villanova, Pennsylvania 19085, United States.
Hannah KesslerDepartment of Chemistry, Villanova University, Villanova, Pennsylvania 19085, United States.
Hannah BrosmanDepartment of Chemistry, Villanova University, Villanova, Pennsylvania 19085, United States.
Kirsten J RuudDepartment of Chemistry and Biotechnology, University of Wisconsin-River Falls, River Falls, Wisconsin 54022, United States.
Alan F FalkowskiDepartment of Chemistry and Biotechnology, University of Wisconsin-River Falls, River Falls, Wisconsin 54022, United States.
Constance ViolletDepartment of Chemistry, Villanova University, Villanova, Pennsylvania 19085, United States.
Christina R BourneDepartment of Chemistry and Biochemistry, University of Oklahoma, Norman, Oklahoma 73019, United States.ORCID https://orcid.org/0000-0001-6192-3392
Matthew C O'ReillyDepartment of Chemistry, Villanova University, Villanova, Pennsylvania 19085, United States.ORCID https://orcid.org/0000-0002-9175-4179
Villanova University · USUniversity of Wisconsin–River Falls · USUniversity of Oklahoma · US

Funding

Structure-Function Studies of MsvR, a Methanogen-Specific Transcriptional RegulaP20GM103640 · NIGMS · UNIVERSITY OF OKLAHOMA · PI THOMAS, LEONARD M · 2012 to 2021
$20.4M
Development of Allosteric Dihydrofolate Reductase Inhibitors: Exploration of a Novel Inhibitory Mechanism for a Validated Antibiotic TargetR15GM140412 · NIGMS · VILLANOVA UNIVERSITY · PI O'REILLY, MATTHEW C · 2021 to 2021
$341k
NIGMS NIH HHS P20 GM103640NIGMS NIH HHS R15 GM140412
6 · The paper itself

Abstract

Antibiotic resistance among bacteria puts immense strain on public health. The discovery of new antibiotics that work through unique mechanisms is one important pillar toward combating this threat of resistance. A functionalized amino dihydropyrimidine was reported to exhibit antibacterial activity via the inhibition of dihydrofolate reductase, an underexploited antibacterial target. Despite this promise, little is known about its structure-activity relationships (SAR) and mechanism of activity. Toward this goal, the aza-Biginelli reaction was optimized to allow for the preparation of focused libraries of functionalized amino dihydropyridines, which in some cases required the use of variable temperature NMR analysis for the conclusive assignment of compound identity and purity. Antibacterial activity was examined using microdilution assays, and compound interactions with dihydrofolate reductase were assessed using antimicrobial synergy studies alongside

Identifiers

PMID36312355
PMCPMC9607683
OpenAlexW4306153968

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.