ArticleJournal of medicinal chemistry2015
Antibacterial drug leads: DNA and enzyme multitargeting.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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.
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.
Who cites it
17 citing papers in PubMed.
- Amidine containing compounds: Antimicrobial activity and its potential in combating antimicrobial resistance.Heliyon · 2024Review
- Investigating the Antimicrobial Potential of 560 Compounds from the Pandemic Response Box and COVID Box against Resistant Gram-Negative Bacteria.Antibiotics (Basel, Switzerland) · 2024Article
- Small Molecules Incorporating Privileged Amidine Moiety as Potential Hits Combating Antibiotic-Resistant Bacteria.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Escaping ESKAPE resistance:Royal Society open science · 2023Article
- An aromatic imidazoline derived from chloroquinoline triggers cell cycle arrest and inhibits with high selectivity the Trypanosoma cruzi mammalian host-cells infection.PLoS neglected tropical diseases · 2021Article
- Biolayer interferometry provides a robust method for detecting DNA binding small molecules in microbial extracts.Analytical and bioanalytical chemistry · 2021Article
- A polymeric approach toward resistance-resistant antimicrobial agent with dual-selective mechanisms of action.Science advances · 2021Article
- Modeling antimalarial and antihuman African trypanosomiasis compounds: a ligand- and structure-based approaches.Molecular diversity · 2020Article
- Discovery of Lipophilic Bisphosphonates That Target Bacterial Cell Wall and Quinone Biosynthesis.Journal of medicinal chemistry · 2019Article
- Three-Component Reaction of Benzylamines, Diethyl Phosphite and Triethyl Orthoformate: Dependence of the Reaction Course on the Structural Features of the Substrates and Reaction Conditions.Molecules (Basel, Switzerland) · 2017Article
- Pentamidine sensitizes Gram-negative pathogens to antibiotics and overcomes acquired colistin resistance.Nature microbiology · 2017Article
- Antileishmanial Mechanism of Diamidines Involves Targeting Kinetoplasts.Antimicrobial agents and chemotherapy · 2016Article
- Efficient O-Functionalization of Carbohydrates with Electrophilic Reagents.Angewandte Chemie (International ed. in English) · 2016Article
- Structure and Function of a "Head-to-Middle" Prenyltransferase: Lavandulyl Diphosphate Synthase.Angewandte Chemie (International ed. in English) · 2016Article
- Mixed up minor groove binders: Convincing A·T specific compounds to recognize a G·C base pair.Bioorganic & medicinal chemistry letters · 2015Article
- Antagonism screen for inhibitors of bacterial cell wall biogenesis uncovers an inhibitor of undecaprenyl diphosphate synthase.Proceedings of the National Academy of Sciences of the United States of America · 2015Article
- In Vitro and in Vivo Activity of Multitarget Inhibitors against Trypanosoma brucei.ACS infectious diseases · 2015Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
10 authors.
Funding
Abstract
We report the results of an investigation of the activity of a series of amidine and bisamidine compounds against Staphylococcus aureus and Escherichia coli. The most active compounds bound to an AT-rich DNA dodecamer (CGCGAATTCGCG)2 and using DSC were found to increase the melting transition by up to 24 °C. Several compounds also inhibited undecaprenyl diphosphate synthase (UPPS) with IC50 values of 100-500 nM, and we found good correlations (R(2) = 0.89, S. aureus; R(2) = 0.79, E. coli) between experimental and predicted cell growth inhibition by using DNA ΔTm and UPPS IC50 experimental results together with one computed descriptor. We also solved the structures of three bisamidines binding to DNA as well as three UPPS structures. Overall, the results are of general interest in the context of the development of resistance-resistant antibiotics that involve multitargeting.
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Registered trials
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.