ArticleBioorganic & medicinal chemistry letters2020
Addition of ethylamines to the phenols of bithionol and synthetic retinoids does not elicit activity in gram-negative bacteria.
Article in Bioorganic & medicinal chemistry letters, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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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.
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Who cites it
4 citing papers in PubMed.
- Evaluation of the Multivalent Immunoprotective Effects of Protein, DNA, and IgY Vaccines AgainstInternational journal of molecular sciences · 2025Article
- Using membrane perturbing small molecules to target chronic persistent infections.RSC medicinal chemistry · 2021Review
- Synthesis and biological evaluation of an antibacterial azaborine retinoid isostereTetrahedron letters · 2021Article
- Repurposing Clinically Approved Drugs for the Treatment ofACS omega · 2020Article
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Authors and funding
5 authors.
Funding
Abstract
Our labs have demonstrated the activity of bithionol and synthetic retinoids against methicillin-resistant Staphylococcus aureus (MRSA), as well as their membrane-acting mechanism of action. However, the compounds lack activity in gram-negative species. Herein, we apply a known strategy for converting gram-positive agents into broad-spectrum therapies: addition of an alkylamine. By appending an alkylamine to the phenols of these known membrane disruptors, we test whether this approach is applicable to our compounds. Ultimately, biological testing in four MRSA strains and three gram-negative species showed abolished or diminished activity in all our analogs compared to their parent compounds and no gram-negative activity. Thus, we find that alkylamines would not elicit broad-spectrum activity from bithionol or CD437 derivatives.
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