ArticleEuropean journal of medicinal chemistry2010
Synthesis and structure activity relationship studies of novel Staphylococcus aureus Sortase A inhibitors.
Article in European journal of medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 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
9 citing papers in PubMed, 28 citations in OpenAlex.
- Structural and functional insights of sortases and their interactions with antivirulence compounds.Current research in structural biology · 2024Review
- Identification of Novel Antistaphylococcal Hit Compounds Targeting Sortase A.Molecules (Basel, Switzerland) · 2021Article
- Targeting Bacterial Sortases in Search of Anti-Virulence Therapies with Low Risk of Resistance Development.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Sorting out the Superbugs: Potential of Sortase A Inhibitors among Other Antimicrobial Strategies to Tackle the Problem of Antibiotic Resistance.Antibiotics (Basel, Switzerland) · 2021Article
- Taxifolin, an Inhibitor of Sortase A, Interferes With the Adhesion of Methicillin-ResistantFrontiers in microbiology · 2021Article
- Design and Synthesis of Small Molecules as PotentAntibiotics (Basel, Switzerland) · 2020Review
- Asymmetric Disulfanylbenzamides as Irreversible and Selective Inhibitors of Staphylococcus aureus Sortase A.ChemMedChem · 2020Article
- In Situ Cyclization of Native Proteins: Structure-Based Design of a Bicyclic Enzyme.Angewandte Chemie (International ed. in English) · 2018Article
- Structural Analysis of Sortase A Inhibitors.Molecules (Basel, Switzerland) · 2016Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Synthetic methods have been developed for lead Sortase A inhibitors identified from previous studies. Several derivatives of the lead inhibitor were synthesized to derive preliminary structure activity relationships (SAR). Different regions of the lead inhibitor that are critical for the enzyme activity have been determined by systematic SAR studies. The E stereochemistry of the lead compound was found to be critical for its activity. Replacement of the E double bond with Z double bond or a rigid triple bond reduced the enzyme inhibitory activity in most cases. Reduction of the double bond to a C-C single bond resulted in complete loss of activity. Amide carbonyl and NH groups were also found to be crucial for the activity of this class of inhibitors, as well. The morpholine ring oxygen atom was also found to be an important factor for the activity of the lead inhibitor. Preliminary SAR studies led to the identification of compounds with improved enzyme inhibition. The most active compound was found to have an IC(50) value of 58 microM against the enzyme.
Indexed as
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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.