Structure-activity relationship studies of [1,2,5]oxadiazolo[3,4-b]pyrazine-containing polymyxin-selective resistance-modifying agents.

Somnath Dutta, Nianzi Liu, Yuefeng Gao, Lily Beck, Xiang Wang

Abstract read

In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it

0cells of the map it votes in

1citing 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

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3 · Its place in the literature

Who cites it

1 citing paper in PubMed.

Synthesis, crystal structure and Hirshfeld surface analysis of (3Acta crystallographica. Section E, Crystallographic communications · 2024
Article

4 · The record

Corrections and comments

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5 · Who and what money

Authors and funding

5 authors.

Somnath DuttaDepartment of Chemistry, University of Colorado, Boulder, CO 80309, USA.

Nianzi LiuDepartment of Chemistry, University of Colorado, Boulder, CO 80309, USA.

Yuefeng GaoDepartment of Chemistry, University of Colorado, Boulder, CO 80309, USA.

Lily BeckDepartment of Chemistry, University of Colorado, Boulder, CO 80309, USA.

Xiang WangDepartment of Chemistry, University of Colorado, Boulder, CO 80309, USA. Electronic address: xiang.wang@colorado.edu.

Funding

Development of Novel Resistance-Modifying Agents for MRSAR33AI121581 · NIAID · UNIVERSITY OF COLORADO · PI WANG, XIANG · 2018 to 2020

$1.4M

NIAID NIH HHS R33 AI121581

6 · The paper itself

Abstract

Multidrug-resistant (MDR) Gram-negative bacteria are an urgent and rapidly spreading threat to human health with limited treatment options. Previously, we discovered a novel [1,2,5]oxadiazolo[3,4-b]pyrazine-containing compound (1) that selectively re-sensitized a variety of MDR Gram-negative bacteria to colistin, one of the last-resort antibiotic. Herein, we report the structure-activity relationship studies of compound 1 that led to the discovery of several more potent and/or less toxic resistance-modifying agents (RMAs). Further evaluation of these RMAs showed that they were effective in a wide range of MDR bacteria. These results demonstrated these compounds as a novel class of RMAs and may be further developed as therapeutic agents.

Indexed as

Gram-Negative Bacterial InfectionsPolymyxinsAnti-Bacterial AgentsDrug Resistance, Multiple, BacterialGram-Negative BacteriaHumansMicrobial Sensitivity TestsPyrazinesStructure-Activity RelationshipAnti-Bacterial AgentsPolymyxinsPyrazinesAntimicrobial resistanceColistinMultidrug-resistant bacteriaPolymyxinResistance-modifying agentsStructure-activity relationship

Identifiers

PMID35788034

DOI10.1016/j.bmcl.2022.128878

PMCPMC10101151

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