Solid-phase synthesis development of a thymidinyl and 2′-deoxyuridinyl Ugi library for anti-bacterial agent screening

A solid-phase synthesis has been developed to make a thymidinyl and 2′-deoxyuridinyl Ugi library starting from 5′-azidonucleosides loaded onto polystyrene butyl diethylsilane (PS-DES) resin. Library synthesis development including: Ugi reaction optimization; selection of building blocks and optimization to 96-well filter plate synthesis are reported. A 1344 member library was synthesized for anti-bacterial screening.