ArticleJournal of medicinal chemistry2017
Synthesis and Biological Evaluation of Bile Acid Analogues Inhibitory to Clostridium difficile Spore Germination.
Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
25 citing papers in PubMed, 42 citations in OpenAlex.
- Biofilm- and Spore-Disruptive Star-Shaped Poly(l-lysine)/Hyaluronic Acid Microgels for Targeted Oral Therapy ofBiomacromolecules · 2026Article
- 5,6-Fused heterocycle cholate derivatives as spore germination inhibitors of Clostridioides difficile.Bioorganic & medicinal chemistry · 2026Article
- Structure-guided design of a synthetic bile acid that inhibits Clostridioides difficile TcdB toxin.Nature microbiology · 2025Article
- Targeting SleC and CspB in the Inhibition of Spore Germination inJournal of medicinal chemistry · 2025Article
- Advances in Pharmacological Activities, Biosynthesis, and Structural Modification of Ursodeoxycholic Acid (UDCA): A Review.Drug design, development and therapy · 2025Review
- Current and Ongoing Developments in TargetingMicroorganisms · 2024Review
- The design, synthesis, and inhibition of Clostridioides difficile spore germination by acyclic and bicyclic tertiary amide analogs of cholate.European journal of medicinal chemistry · 2023Article
- Mechanism of germination inhibition of Clostridioides difficile spores by an aniline substituted cholate derivative (CaPA).The Journal of antibiotics · 2023Article
- Trust Your Gut: Strategies and Tactics for Intestinally Restricted Drugs.ACS medicinal chemistry letters · 2023Review
- Design and synthesis of bile acid derivatives and their activity against colon cancer.RSC medicinal chemistry · 2022Article
- Studies on the Importance of the 7α-, and 12α- hydroxyl groups of N-Aryl-3α,7α,12α-trihydroxy-5β-cholan-24-amides on their Antigermination Activity Against a Hypervirulent Strain of Clostridioides (Clostridium) difficile.Bioorganic & medicinal chemistry · 2021Article
- Article
- Opportunities for Nanomedicine inAntibiotics (Basel, Switzerland) · 2021Review
- Structural modifications that increase gut restriction of bile acid derivatives.RSC medicinal chemistry · 2021Article
- Synthesis of new bile acid-fused tetrazoles using the Schmidt reaction.Beilstein journal of organic chemistry · 2021Article
- Pharmacokinetics of CamSA, a potential prophylactic compound against Clostridioides difficile infections.Biochemical pharmacology · 2021Article
- The Great ESKAPE: Exploring the Crossroads of Bile and Antibiotic Resistance in Bacterial Pathogens.Infection and immunity · 2020Review
- Review
- The Design, Synthesis, and Characterizations of Spore Germination Inhibitors Effective against an Epidemic Strain of Clostridium difficile.Journal of medicinal chemistry · 2018Article
- Novel FR-900493 Analogues That Inhibit the Outgrowth ofACS omega · 2018Article
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
Abstract
Standard antibiotic-based strategies for the treatment of Clostridium difficile infections disrupt indigenous microbiota and commonly fail to eradicate bacterial spores, two key factors that allow recurrence of infection. As an alternative approach to controlling C. difficile infection, a series of bile acid derivatives have been prepared that inhibit taurocholate-induced spore germination. These analogues have been evaluated in a highly virulent NAP1 strain using optical density and phase-contrast microscopy assays. Heterocycle substitutions at C24 were well-tolerated and several tetrazole-containing derivatives were highly potent inhibitors in both assays, with complete inhibition of spore germination observed at 10-25 μM. To limit intestinal absorption, C7-sulfated analogues designed to avoid active and passive transport pathways were prepared. One of these derivatives, compound 21b, was found to be a potent inhibitor of C. difficile spore germination and poorly permeable in a Caco-2 model of intestinal epithelial absorption, suggesting that it is likely to be gut-restricted.
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What OpenQuestion holds
Registered trials
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.