Gram Scale Synthesis of Membrane-Active Antibacterial 4-Quinolone Lead Compound.

Gorakhnath R Jachak, Moyosore O Orimoloye, Courtney C Aldrich

Abstract read

In one paragraph

Article in The Journal of organic chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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0cells of the map it votes in

0citing 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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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

3 authors.

Gorakhnath R JachakDepartment of Medicinal Chemistry, University of Minnesota, Minneapolis, Minnesota 55455, United States.

Moyosore O OrimoloyeDepartment of Medicinal Chemistry, University of Minnesota, Minneapolis, Minnesota 55455, United States.ORCID 0000-0002-0330-008X

Courtney C AldrichDepartment of Medicinal Chemistry, University of Minnesota, Minneapolis, Minnesota 55455, United States.ORCID 0000-0001-9261-594X

Funding

Membrane-active quinoline and quinazoline antibacterials that target Gram positive pathogensR01AI146116 · NIAID · DARTMOUTH COLLEGE · PI CHEUNG, AMBROSE LIN YAU · 2020 to 2024

$3.9M

Optimization of a novel compound that enhances the activity of beta-lactams against Gram+ bacteriaR21AI130540 · NIAID · DARTMOUTH COLLEGE · PI CHEUNG, AMBROSE LIN YAU · 2017 to 2018

$449k

NIAID NIH HHS R01 AI146116NIAID NIH HHS R21 AI130540

6 · The paper itself

Abstract

An improved method for the synthesis of a new quinolone class of antibiotics, which are exceptionally potent against gram-positive bacteria, has been developed and the structure confirmed by single-crystal X-ray analysis. In the course of synthesis, using either Chan-Lam coupling or Buchwald-Hartwig amination, we have shown that the careful choice of protecting group at the C4 position of the quinoline is required for selective amination at the C5 position and subsequent deprotection to avoid the formation of a novel pyrido[4,3,2-

Indexed as

Quinolones4-QuinolonesAnti-Bacterial AgentsGram-Positive BacteriaStructure-Activity Relationship4-QuinolonesAnti-Bacterial AgentsQuinolones

Identifiers

PMID37071556

DOI10.1021/acs.joc.3c00239

PMCPMC10733119

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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.