ArticleMolecules (Basel, Switzerland)2015
Antibacterial barbituric acid analogues inspired from natural 3-acyltetramic acids; synthesis, tautomerism and structure and physicochemical property-antibacterial activity relationships.
Article in Molecules (Basel, Switzerland), 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- Novel Steroidal (Thio)barbiturate Hybrids: From Design to Preclinical Assessment in Tumor Therapy.ChemMedChem · 2026Article
- Conformational analysis of different tautomers of some antibiotics.Journal of molecular modeling · 2026Article
- Advances in Antimicrobial Applications of Ag, Cu, and AgCu Nanoparticle-Doped Polymeric Composite Materials: A Comprehensive Review.ACS nano · 2025Review
- Proline-Hinged α-Helical Peptides Sensitize Gram-Positive Antibiotics, Expanding Their Physicochemical Properties to Be Used as Gram-Negative Antibiotics.Journal of medicinal chemistry · 2024Article
- Molecular Diversity via Tetrasubstituted Alkenes Containing a Barbiturate Motif: Synthesis and Biological Activity.Molecules (Basel, Switzerland) · 2020Article
- Article
- Nematicidal Activity of 3-Acyltetramic Acid Analogues Against Pine Wood Nematode, Bursaphelenchus xylophilus.Molecules (Basel, Switzerland) · 2017Article
- Larvicidal and Nematicidal Activities of 3-Acylbarbituric Acid Analogues against Asian Tiger Mosquito, Aedes albopictus, and Pine Wood Nematode, Bursaphelenchus xylophilus.Molecules (Basel, Switzerland) · 2017Article
Corrections and comments
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Authors and funding
2 authors.
Funding
Abstract
The synthesis, tautomerism and antibacterial activity of novel barbiturates is reported. In particular, 3-acyl and 3-carboxamidobarbiturates exhibited antibacterial activity, against susceptible and some resistant Gram-positive strains of particular interest is that these systems possess amenable molecular weight, rotatable bonds and number of proton-donors/acceptors for drug design as well as less lipophilic character, with physicochemical properties and ionic states that are similar to current antibiotic agents for oral and injectable use. Unfortunately, the reduction of plasma protein affinity by the barbituric core is not sufficient to achieve activity in vivo. Further optimization to reduce plasma protein affinity and/or elevate antibiotic potency is therefore required, but we believe that these systems offer unusual opportunities for antibiotic drug discovery.
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