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Chemical Structure| 1258453-75-6 Chemical Structure| 1258453-75-6

Structure of Obefazimod
CAS No.: 1258453-75-6

Chemical Structure| 1258453-75-6

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ABX-464 is an inhibitor of the HIV replication potentially for the treatment of HIV infection.

Synonyms: Abx464; SPL-464; BX-464

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Stolz, Brice J ; Abouelkhair, Ahmed A ; Seleem, Mohamed N ;

Abstract: Clostridioides difficile is a major cause of nosocomial infections, often associated with individuals who have gut dysbiosis from previous antibiotic therapies. C. difficile infections (CDI) have a high recurrence rate and impose significant financial and mortality burdens on the healthcare system. Therefore, novel anti-C. difficile drugs are urgently needed to treat and reduce the severity and recurrence of infection. In this study, we screened a library of 618 antiviral drugs to identify a potential candidate for repurposing as novel anti-C. difficile therapeutics. Following our preliminary screening, we identified 9 novel compounds that inhibited C. difficile at a concentration of 16 μM or lower. Among these, 4 antiviral compounds demonstrated the most potent anti-C. difficile activity against a panel of 15 C. difficile isolates, with minimum inhibitory concentrations (MICs) comparable to the drug of choice, vancomycin. These include rottlerin (MIC50 = 0.25 μg/mL), α-mangostin (MIC50 = 1 μg/mL), dryocrassin ABBA (MIC50 = 1 μg/mL), and obefazimod (MIC50 = 4 μg/mL). All exhibited minimal to no activity against representative members of the human gut microbiota. Interestingly, α-mangostin, a natural xanthone derived from the mangosteen fruit, exhibited strong bactericidal action, clearing a high inoculum of C. difficile in less than an hour. All other drugs exhibited bacteriostatic activity. Given their characteristics, these compounds show great promise as novel treatments for CDI.

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Stolz, Brice Jasarino ; Seleem, Mohamed N ; Abouelkhair, Ahmed A ;

Abstract: Clostridium difficile (C. difficile) is a major cause of nosocomial infections, often associated with individuals who have gut dysbiosis from previous therapies. C. difficile infections have a high recurrence rate and impose significant financial and mortality burdens on the healthcare system. Novel anti-C. difficile drugs are urgently needed to treat and reduce the severity and recurrence of infection. In this study, we screened a library of 618 antiviral drugs to identify a potential candidate for repurposing as novel anti-C. difficile treatments. Following our preliminary screening, we identified 9 novel compounds that inhibit C. difficile at a concentration of 16 µM or lower. Among these, 4 antiviral compounds demonstrated the most potent anti-C. difficile activity against a panel of 15 C. difficile isolates, with minimum inhibitory concentrations (MICs) comparable to the drug of choice, . These include (MIC50 = 0.25 µg/mL), (MIC50 = 1 µg/mL), (MIC50 = 1 µg/mL), and (MIC50 = 4 µg/mL). All exhibited minimal to no activity against representative members of the gut microbiota. Interestingly, α-mangostin, a natural xanthone derived from the mangosteen fruit, exhibited strong bactericidal action, clearing a high inoculum of C. difficile in less than an hour. All other drugs exhibited bacteriostatic activity. Given the characteristics of these compounds, they show great promise as novel treatments for CDI.

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Product Details of Obefazimod

CAS No. :1258453-75-6
Formula : C16H10ClF3N2O
M.W : 338.71
SMILES Code : FC(F)(F)OC1=CC=C(NC2=NC3=C(Cl)C=CC=C3C=C2)C=C1
Synonyms :
Abx464; SPL-464; BX-464
MDL No. :MFCD31657325
InChI Key :OZOGDCZJYVSUBR-UHFFFAOYSA-N
Pubchem ID :49846599

Safety of Obefazimod

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501

Isoform Comparison

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.95mL

0.59mL

0.30mL

14.76mL

2.95mL

1.48mL

29.52mL

5.90mL

2.95mL

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