Bis-Cyclic-Guanidine as a Novel Class of Compounds Potent Against Clostridium Difficile.

Bis-Cyclic-Guanidine as a Novel Class of Compounds Potent Against Clostridium Difficile. ChemMedChem. 2018 May 16;: Authors: Li C, Teng P, Peng Z, Sang P, Sun X, Cai J Abstract Clostridium difficile infection (CDI) symptoms range from diarrhea to severe toxic megacolon and even death. Due to its rapid acquisition of resistance, C. difficile is listed as an urgent antibiotic-resistant threat, and has surpassed methicillin-resistant Staphylococcus aureus (MRSA) as the most common hospital-acquired infections in the USA. To combat the pathogen, the new structural class of pseudo peptides that exhibit antimicrobial activities could play an important role. Herein, we report that bis-cyclic guanidine compounds that exhibit potent antibacterial activity against C. difficile with decent selectivity. Eight compounds showed high in vitro potency against C. difficile UK6 with MIC of 1.0 μg/mL, and cytotoxic selectivity index (SI) up to 37. Moreover, the most selective compound 13 is also effective upon the treatment of C. difficile-induced diseases in the mouse model of CDI, and appears to be a very promising new candidate for the treatment of CDI. PMID: 29768720 [PubMed - as supplied by publisher]
Source: ChemMedChem - Category: Chemistry Authors: Tags: ChemMedChem Source Type: research