Bis-Cyclic Guanidines as a Novel Class of Compounds Potent against Clostridium difficile.

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 infection in the USA. To combat this pathogen, a new structural class of pseudo-peptides that exhibit antimicrobial activities could play an important role. Herein we report a set of bis-cyclic guanidine compounds that show potent antibacterial activity against C. difficile with decent selectivity. Eight compounds showed high in vitro potency against C. difficile UK6 with MIC values of 1.0 μg mL^-1 , and cytotoxic selectivity index (SI) values up to 37. Moreover

SUBMITTER: Li C 

PROVIDER: S-EPMC6121702 | biostudies-literature | 2018 Jul

REPOSITORIES: biostudies-literature