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

Author: Ohkawa T.   Goto S.   Miki S.   Sato A.   Kuroda T.   Iwatani K.   Takeuchi M.   Nakano M.  

Publisher: Informa Healthcare

ISSN: 1366-5928

Source: Xenobiotica, Vol.28, Iss.9, 1998-09, pp. : 877-886

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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.

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