Function‐Oriented Synthesis of Liponucleoside Antibiotics

Abstract

Abstract Function‐oriented synthesis of a class of liponucleoside antibiotics was investigated through rational simplification guided by previous structure–activity relationship studies of caprazamycins and muraymycins to address the issue associated with their molecular complexity. A lactam‐fused isoxazolidine scaffold was designed, and a diverse set of lactam‐fused isoxazolidines derivatives were constructed by intramolecular 1,3‐dipolar cycloaddition of alkenyl nitrones. Several analogues exhibited moderate activity against a range of Gram‐positive drug‐resistant bacterial pathogens.