ArticleACS medicinal chemistry letters2015
Improved Synthesis of Biotinol-5'-AMP: Implications for Antibacterial Discovery.
Article in ACS medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed.
- A broad inhibitor of acyl-acyl carrier protein synthetases.Biochemistry and biophysics reports · 2023Article
- Repurposed inhibitor of bacterial dihydrodipicolinate reductase exhibits effective herbicidal activity.Communications biology · 2023Article
- Structural Study of Potent Triazole-Based Inhibitors ofACS medicinal chemistry letters · 2023Article
- An environment-friendly methodology for the construction of diversified bicycloacenaphtho[1,2-d]imidazole-8-thione scaffolds using spinel NiFeMolecular diversity · 2022Article
- Advanced Resistance Studies Identify Two Discrete Mechanisms inAntibiotics (Basel, Switzerland) · 2020Article
- The Biotin Biosynthetic Pathway in Mycobacterium tuberculosis is a Validated Target for the Development of Antibacterial Agents.Current medicinal chemistry · 2020Review
- Native mass spectrometry identifies an alternative DNA-binding pathway for BirA from Staphylococcus aureus.Scientific reports · 2019Article
- New Series of BPL Inhibitors To Probe the Ribose-Binding Pocket ofACS medicinal chemistry letters · 2016Article
- Biotin Protein Ligase Is a Target for New Antibacterials.Antibiotics (Basel, Switzerland) · 2016Review
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Authors and funding
13 authors.
Funding
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Abstract
An improved synthesis of biotinol-5'-AMP, an acyl-AMP mimic of the natural reaction intermediate of biotin protein ligase (BPL), is reported. This compound was shown to be a pan inhibitor of BPLs from a series of clinically important bacteria, particularly Staphylococcus aureus and Mycobacterium tuberculosis, and kinetic analysis revealed it to be competitive against the substrate biotin. Biotinol-5'-AMP also exhibits antibacterial activity against a panel of clinical isolates of S. aureus and M. tuberculosis with MIC values of 1-8 and 0.5-2.5 μg/mL, respectively, while being devoid of cytotoxicity to human HepG2 cells.
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