Rationally Designed Novel Phenyloxazoline Synthase Inhibitors: Chemical Synthesis and Biological Evaluation to Accelerate the Discovery of New Antimycobacterial Antibiotics.
Article in Molecules (Basel, Switzerland), 2023. 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
0.5field-weighted citation impact, top 30% 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
1 citing paper in PubMed, 2 citations in OpenAlex.
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
12 authors at 5 institutions in 2 countries.
Mousumi ShyamDepartment of Pharmaceutical Sciences & Technology, Birla Institute of Technology, Mesra, Ranchi 835215, India.
Gourab BhattacharjeDepartment of Biotechnology, Indian Institute of Technology Kharagpur, Kharagpur 721302, India.ORCID 0000-0001-7823-8033
Chris DanielMycobacteria Research Laboratory, School of Natural Sciences, Institute of Structural and Molecular Biology, Birkbeck, University of London, Malet Street, London WC1E 7HX, UK.ORCID 0000-0002-8650-516X
Amrendra KumarDivision of Medicinal & Process Chemistry, CSIR-Central Drug Research Institute, Sector 10 Janakipuram Extension, Sitapur Road, Lucknow 226031, India.
Pragya YadavDivision of Medicinal & Process Chemistry, CSIR-Central Drug Research Institute, Sector 10 Janakipuram Extension, Sitapur Road, Lucknow 226031, India.
Piyali MukherjeeDepartment of Microbiology and Cell Biology, Centre for Infectious Disease Research, Indian Institute of Science, CV Raman Avenue, Bengaluru 560012, India.
Samsher SinghDepartment of Microbiology and Cell Biology, Centre for Infectious Disease Research, Indian Institute of Science, CV Raman Avenue, Bengaluru 560012, India.
Amit Kumar DasDepartment of Biotechnology, Indian Institute of Technology Kharagpur, Kharagpur 721302, India.ORCID 0000-0001-9703-1898
Tadigoppula NarenderDivision of Medicinal & Process Chemistry, CSIR-Central Drug Research Institute, Sector 10 Janakipuram Extension, Sitapur Road, Lucknow 226031, India.
Amit SinghDepartment of Microbiology and Cell Biology, Centre for Infectious Disease Research, Indian Institute of Science, CV Raman Avenue, Bengaluru 560012, India.ORCID 0000-0001-6761-1664
Venkatesan JayaprakashDepartment of Pharmaceutical Sciences & Technology, Birla Institute of Technology, Mesra, Ranchi 835215, India.
Sanjib BhaktaMycobacteria Research Laboratory, School of Natural Sciences, Institute of Structural and Molecular Biology, Birkbeck, University of London, Malet Street, London WC1E 7HX, UK.ORCID 0000-0002-1165-9295
Central Drug Research Institute · INIndian Institute of Science Bangalore · INBirla Institute of Technology, Mesra · INIndian Institute of Technology Kharagpur · INInstitute of Structural and Molecular Biology · GB
Funding
No grant is acknowledged in the PubMed record.
6 · The paper itself
Abstract
The uncontrolled spread of drug-resistant tuberculosis (DR-TB) clinical cases necessitates the urgent discovery of newer chemotypes with novel mechanisms of action. Here, we report the chemical synthesis of rationally designed novel transition-state analogues (TSAs) by targeting the cyclization (Cy) domain of phenyloxazoline synthase (MbtB), a key enzyme of the conditionally essential siderophore biosynthesis pathway. Following bio-assay-guided evaluation of TSA analogues preferentially in iron-deprived and iron-rich media to understand target preferentiality against a panel of pathogenic and non-pathogenic mycobacteria strains, we identified a hit, i.e.,
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.
Rationally Designed Novel Phenyloxazoline Synthase Inhibitors: Chemical Synthesis and Biological Evaluation to Accelerate the Discovery of New Antimycobacterial Antibiotics. · full record | OpenQuestion