ArticleBioorganic & medicinal chemistry2026
5,6-Fused heterocycle cholate derivatives as spore germination inhibitors of Clostridioides difficile.
Article in Bioorganic & medicinal chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
What it found
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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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
3 citing papers in PubMed.
- Effects of sexual dimorphism and estrous cycle on murineInfection and immunity · 2026Article
- Novel bile salt analogs reduce lipid accumulation in liver cells with potential to treat both metabolic dysfunction-associated steatotic liver disease and Clostridioides difficile infection.bioRxiv : the preprint server for biology · 2026Article
- Bile Acid Analogs with Anti-Germination Activities for Prophylaxis ofBiomolecules · 2025Article
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
Clostridioides difficile is an anaerobic bacterium that is responsible for most antibiotic-associated cases of diarrhea. Clostridioides difficile infection (CDI) begins with the ingestion of an environmentally stable spore that germinates within the GI tract if the concentration and composition of bile salts, ions, and amino acids are favorable. We have shown that the bile salt analog N-phenyl-cholan-24-amide (1) can inhibit spore germination and prevent CDI in animal models of infection. Unfortunately, 1, while stable in the gut of antibiotic-treated animals, is rapidly degraded by normal gastrointestinal microbiota to release cholate and aniline. This instability prevents its use as a prophylactic for CDI. To generate more stable bile salt analogs, we removed the amide by either reducing it to an amine or converting it into 5,6-fused heterocycles. We found that reduction of the amide to an amine resulted in a significant loss of activity, but cyclization to benzimidazole (6a), benzothiazole (6b), or benzoxazole (6c) gave anti-germinants with good IC
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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.