A novel agent effective against Clostridium difficile infection.
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.
GLSynthesis, Inc Worcester, Massachusetts, USA.
Sofya
S
Dvoskin
Wei-Chu
WC
Xu
Neal C
NC
Brown
Ivan B
IB
Yanachkov
Milka
M
Yanachkova
George E
GE
Wright
D000284:Administration, Oral; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000627:therapeutic use; D016360:Clostridioides difficile / Q000187:drug effects* / Q000502:physiology; D006224:Cricetinae; D004259:DNA-Directed DNA Polymerase / Q000378:metabolism; D004195:Disease Models, Animal; D004761:Enterocolitis, Pseudomembranous / Q000188:drug therapy* / Q000382:microbiology / Q000401:mortality; D005260:Female; D006801:Humans; D009025:Morpholines / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000627:therapeutic use; D019384:Nucleic Acid Synthesis Inhibitors; D011687:Purines / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000627:therapeutic use; D014640:Vancomycin / Q000008:administration & dosage / Q000627:therapeutic use
D000900:Anti-Bacterial Agents; D009025:Morpholines; D019384:Nucleic Acid Synthesis Inhibitors; D011687:Purines; D014640:Vancomycin; D004259:DNA-Directed DNA Polymerase