Structural determination of metabolites of S-1153, a new, potent, non-nucleoside, anti-HIV agent in rat liver microsomes

Abstract

1. S-1153, a non-nucleoside agent that is under development in the USA as a new antiHIV agent, has potent antiviral activity based on the inhibition of reverse transcriptase. 2. S-1153wasincubatedwithratliver microsomes andNADPH,andsevenmetabolites were formed. The main metabolites were identified as the S -oxide, N -oxide and sulphone of S-1153. 3. Two other minor metabolites were assumed to be S-1153 hydroxylated on the isopropyl moiety. 4. Our findings confirmed the existence of at least three oxidative metabolic pathways of S-1153.