ArticleActa crystallographica. Section F, Structural biology communications2015
Crystallographic insights into the structure-activity relationships of diazaborine enoyl-ACP reductase inhibitors.
Article in Acta crystallographica. Section F, Structural biology communications, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 20 citations in OpenAlex.
- Underexplored Ligand-Binding Features of FabI From Staphylococcus aureus and Escherichia coli: A Comparative Pharmacophoric Modeling and Surface Mapping Approach.ChemMedChem · 2026Article
- Hybrid Isoxazole-Hydroxyapatite composites as antimicrobial agents: integrated in silico and in vitro investigation.Journal of materials science. Materials in medicine · 2026Article
- Rediscovering Diazaborines: Synthesis and Bioactivity Profiling of Boron-Containing FabI Inhibitors against Gram-Negative Bacteria.Journal of medicinal chemistry · 2026Article
- The Boron Advantage: The Evolution and Diversification of Boron's Applications in Medicinal Chemistry.Pharmaceuticals (Basel, Switzerland) · 2022Review
- A Novel Benzoxaborole Is Active against Escherichia coli and Binds to FabI.Antimicrobial agents and chemotherapy · 2021Article
- The genome of a Bacteroidetes inhabitant of the human gut encodes a structurally distinct enoyl-acyl carrier protein reductase (FabI).The Journal of biological chemistry · 2020Article
- Identification of cellular targets of a series of boron heterocycles using TIPA II-A sensitive target identification platform.Bioorganic & medicinal chemistry · 2016Article
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
Abstract
Enoyl-ACP reductase, the last enzyme of the fatty-acid biosynthetic pathway, is the molecular target for several successful antibiotics such as the tuberculosis therapeutic isoniazid. It is currently under investigation as a narrow-spectrum antibiotic target for the treatment of several types of bacterial infections. The diazaborine family is a group of boron heterocycle-based synthetic antibacterial inhibitors known to target enoyl-ACP reductase. Development of this class of molecules has thus far focused solely on the sulfonyl-containing versions. Here, the requirement for the sulfonyl group in the diazaborine scaffold was investigated by examining several recently characterized enoyl-ACP reductase inhibitors that lack the sulfonyl group and exhibit additional variability in substitutions, size and flexibility. Biochemical studies are reported showing the inhibition of Escherichia coli enoyl-ACP reductase by four diazaborines, and the crystal structures of two of the inhibitors bound to E. coli enoyl-ACP reductase solved to 2.07 and 2.11 Å resolution are reported. The results show that the sulfonyl group can be replaced with an amide or thioamide without disruption of the mode of inhibition of the molecule.
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