ArticleJournal of medicinal chemistry2012
Coumarin-based inhibitors of Bacillus anthracis and Staphylococcus aureus replicative DNA helicase: chemical optimization, biological evaluation, and antibacterial activities.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 66 citations in OpenAlex.
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- Synthesis, Antimicrobial Activity, and Tyrosinase Inhibition by Multifunctional 3,4-Dihydroxy-Phenyl Peptidomimetics.International journal of molecular sciences · 2025Article
- Mystery of the Passerini Reaction for the Synthesis of the Antimicrobial Peptidomimetics against Nosocomial Pathogenic Bacteria.International journal of molecular sciences · 2024Article
- Inhibition of Replication Fork Formation and Progression: Targeting the Replication Initiation and Primosomal Proteins.International journal of molecular sciences · 2023Review
- Phenolic Compounds in Bacterial Inactivation: A Perspective from Brazil.Antibiotics (Basel, Switzerland) · 2023Review
- Effects of Surfactant Volume Fraction on the Antioxidant Efficiency and on The Interfacial Concentrations of Octyl and TetradecylMolecules (Basel, Switzerland) · 2021Article
- Synthesis and molecular docking studies of novel pyrimidine derivatives as potential antibacterial agents.Molecular diversity · 2020Article
- 4,8-Dimethylcoumarin Inhibitors of Intestinal Anion Exchanger slc26a3 (Downregulated in Adenoma) for Anti-Absorptive Therapy of Constipation.Journal of medicinal chemistry · 2019Article
- Blocking the Trigger: Inhibition of the Initiation of Bacterial Chromosome Replication as an Antimicrobial Strategy.Antibiotics (Basel, Switzerland) · 2019Review
- Prenylated flavonoid-enriched fraction from Maclura tinctoria shows biological activity against Staphylococcus aureus and protects Galleria mellonella larvae from bacterial infection.BMC complementary and alternative medicine · 2019Article
- Anti-MRSA Sesquiterpenes from the Semi-Mangrove PlantMarine drugs · 2018Article
- SLC26A3 inhibitor identified in small molecule screen blocks colonic fluid absorption and reduces constipation.JCI insight · 2018Article
- Versatility of 7-Substituted Coumarin Molecules as Antimycobacterial Agents, Neuronal Enzyme Inhibitors and Neuroprotective Agents.Molecules (Basel, Switzerland) · 2017Article
- Coumarin-benzimidazole hybrids as a potent antimicrobial agent: synthesis and biological elevation.The Journal of antibiotics · 2017Article
- Inhibition of T24 and RT4 Human Bladder Cancer Cell Lines by Heterocyclic Molecules.Medical science monitor : international medical journal of experimental and clinical research · 2017Article
- Targeting DNA Replication and Repair for the Development of Novel Therapeutics against Tuberculosis.Frontiers in molecular biosciences · 2017Review
- Synthesis of umbelliferone derivatives inJournal of biological engineering · 2017Article
- Bromomethylthioindole Inspired Carbazole Hybrids as Promising Class of Anti-MRSA Agents.ACS medicinal chemistry letters · 2016Article
- Alternative pre-approved and novel therapies for the treatment of anthrax.BMC infectious diseases · 2016Review
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
Abstract
The increasing prevalence of drug-resistant bacterial infections demands the development of new antibacterials that are not subject to existing mechanisms of resistance. Previously, we described coumarin-based inhibitors of an underexploited bacterial target, namely the replicative helicase. Here we report the synthesis and evaluation of optimized coumarin-based inhibitors with 9-18-fold increased potency against Staphylococcus aureus (Sa) and Bacillus anthracis (Ba) helicases. Compounds 20 and 22 provided the best potency, with IC(50) values of 3 and 1 μM, respectively, against the DNA duplex strand-unwinding activities of both B. anthracis and S. aureus helicases without affecting the single strand DNA-stimulated ATPase activity. Selectivity index (SI = CC(50)/MIC) values against S. aureus and B. anthracis for compound 20 were 33 and 66 and for compound 22 were 20 and 40, respectively. In addition, compounds 20 and 22 demonstrated potent antibacterial activity against multiple ciprofloxacin-resistant MRSA strains, with MIC values ranging between 0.5 and 4.2 μg/mL.
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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.