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

T. OHKAWA Developmental Research Laboratories, Shionogi & Co., Ltd, 3-1-1, Futaba-cho, Toyonaka, Osaka 561-0825, Japan Discovery Research Laboratories I, Shionogi & Co., Ltd, 2-5-1, Mishima, Settsu, Osaka 566-0022, Japan Pharmaceuticals Research & Development Division, Shionogi & Co., Ltd., 12-4-5, Sagisu, Fukushima-ku, Osaka 553-0002, Japan

S. GOTO Developmental Research Laboratories, Shionogi & Co., Ltd, 3-1-1, Futaba-cho, Toyonaka, Osaka 561-0825, Japan Discovery Research Laboratories I, Shionogi & Co., Ltd, 2-5-1, Mishima, Settsu, Osaka 566-0022, Japan Pharmaceuticals Research & Development Division, Shionogi & Co., Ltd., 12-4-5, Sagisu, Fukushima-ku, Osaka 553-0002, Japan

S. MIKI Developmental Research Laboratories, Shionogi & Co., Ltd, 3-1-1, Futaba-cho, Toyonaka, Osaka 561-0825, Japan Discovery Research Laboratories I, Shionogi & Co., Ltd, 2-5-1, Mishima, Settsu, Osaka 566-0022, Japan Pharmaceuticals Research & Development Division, Shionogi & Co., Ltd., 12-4-5, Sagisu, Fukushima-ku, Osaka 553-0002, Japan

A. SATO Developmental Research Laboratories, Shionogi & Co., Ltd, 3-1-1, Futaba-cho, Toyonaka, Osaka 561-0825, Japan Discovery Research Laboratories I, Shionogi & Co., Ltd, 2-5-1, Mishima, Settsu, Osaka 566-0022, Japan Pharmaceuticals Research & Development Division, Shionogi & Co., Ltd., 12-4-5, Sagisu, Fukushima-ku, Osaka 553-0002, Japan

T. KURODA Developmental Research Laboratories, Shionogi & Co., Ltd, 3-1-1, Futaba-cho, Toyonaka, Osaka 561-0825, Japan Discovery Research Laboratories I, Shionogi & Co., Ltd, 2-5-1, Mishima, Settsu, Osaka 566-0022, Japan Pharmaceuticals Research & Development Division, Shionogi & Co., Ltd., 12-4-5, Sagisu, Fukushima-ku, Osaka 553-0002, Japan

K. IWATANI Developmental Research Laboratories, Shionogi & Co., Ltd, 3-1-1, Futaba-cho, Toyonaka, Osaka 561-0825, Japan Discovery Research Laboratories I, Shionogi & Co., Ltd, 2-5-1, Mishima, Settsu, Osaka 566-0022, Japan Pharmaceuticals Research & Development Division, Shionogi & Co., Ltd., 12-4-5, Sagisu, Fukushima-ku, Osaka 553-0002, Japan

M. TAKEUCHI Developmental Research Laboratories, Shionogi & Co., Ltd, 3-1-1, Futaba-cho, Toyonaka, Osaka 561-0825, Japan Discovery Research Laboratories I, Shionogi & Co., Ltd, 2-5-1, Mishima, Settsu, Osaka 566-0022, Japan Pharmaceuticals Research & Development Division, Shionogi & Co., Ltd., 12-4-5, Sagisu, Fukushima-ku, Osaka 553-0002, Japan

M. NAKANO Developmental Research Laboratories, Shionogi & Co., Ltd, 3-1-1, Futaba-cho, Toyonaka, Osaka 561-0825, Japan Discovery Research Laboratories I, Shionogi & Co., Ltd, 2-5-1, Mishima, Settsu, Osaka 566-0022, Japan Pharmaceuticals Research & Development Division, Shionogi & Co., Ltd., 12-4-5, Sagisu, Fukushima-ku, Osaka 553-0002, Japan

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

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

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