Solid Phase Synthesis of a Metronidazole Oligonucleotide Conjugate

Abstract

Direct, solid phase synthesis of an oligonucleotide conjugate of the antibioticdrug metronidazole was accomplished by the phosphoramidite method. Removal ofprotecting groups and cleavage from the controlled pore glass (CPG) solid support wassuccessful using mild conditions (20% Et3N in pyridine, then conc. NH3 (aq) at rt for 30min) whereas standard conditions (conc. NH3 (aq) at 55 °C for 16 h) cleaved the drug.

Keywords

• CPG
• conjugate
• metronidazole
• oligonucleotide
• phosphoramidite
• solid phase.