Abstract
N(2)-(3,4-Dichlorobenzyl)-7-(2-[1-morpholinyl]ethyl)guanine (MorE-DCBG, 362E) is a synthetic purine that selectively inhibits the replication-specific DNA polymerase of Clostridium difficile. MorE-DCBG and its analogs strongly inhibited the growth of a wide variety of C. difficile strains. When administered orally in a hamster model of C. difficile-specific colitis, 362E was as effective as oral vancomycin, the current agent of choice for treating severe forms of the human disease.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Administration, Oral
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Animals
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Anti-Bacterial Agents / administration & dosage*
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / therapeutic use
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Clostridioides difficile / drug effects*
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Clostridioides difficile / physiology
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Cricetinae
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DNA-Directed DNA Polymerase / metabolism
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Disease Models, Animal
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Enterocolitis, Pseudomembranous / drug therapy*
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Enterocolitis, Pseudomembranous / microbiology
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Enterocolitis, Pseudomembranous / mortality
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Female
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Humans
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Morpholines / administration & dosage*
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Morpholines / chemical synthesis
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Morpholines / therapeutic use
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Nucleic Acid Synthesis Inhibitors*
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Purines / administration & dosage*
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Purines / chemical synthesis
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Purines / therapeutic use
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Vancomycin / administration & dosage
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Vancomycin / therapeutic use
Substances
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Anti-Bacterial Agents
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Morpholines
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Nucleic Acid Synthesis Inhibitors
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Purines
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Vancomycin
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DNA-Directed DNA Polymerase