Property-Guided Synthesis of Aza-Tricyclic Indolines: Development of Gold Catalysis En Route.

ABSTRACT: Antibiotic resistance is a worldwide public health threat that needs to be addressed by improved antibiotic stewardship and continuing development of new chemical entities to treat resistant bacterial infections. Compounds that work alongside known antibiotics as combination therapies offer an efficient and sustainable approach to counteract antibiotic resistance in bacteria. Guided by property-based analysis, a series of aza-tricyclic indolines (ATIs) were synthesized to optimize their physiochemical properties as novel combination therapies with β-lactams to treat methicillin-resistant S. aureus (MRSA) infections. A novel and highly efficient gold-catalyzed tandem cyclization was developed to facilitate the synthesis of these ATIs. One guanidine-containing ATI was discovered to po

SUBMITTER: Barbour PM 

PROVIDER: S-EPMC5367856 | biostudies-literature | 2016 Apr

REPOSITORIES: biostudies-literature