Na+-Glucose Cotransporter Inhibitors as Antidiabetics. I. Synthesis and Pharmacological Properties of 4'-Dehydroxyphlorizin Derivatives Based on a New Concept.

K Tsujihara, M HONGU, K SAITO, M INAMASU…

Index: Tsujihara, Kenji; Hongu, Mitsuya; Saito, Kunio; Inamasu, Masanori; Arakawa, Kenji; Oku, Akira; Matsumoto, Mamoru Chemical and Pharmaceutical Bulletin, 1996 , vol. 44, # 6 p. 1174 - 1180

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Citation Number: 84

Abstract

Based on our new concept that inhibitors of the Na+-glucose contransporter (SGLT) would be useful as antidiabetics, 4'-dehydroxyphlorizin derivatives 1a-f were designed, synthesized, and examined for various pharmacological properties related to antidiabetic activity. In normal rats, 1a, e and phlorizin showed a strong SGLT-inhibitory effect and significantly increased urinary glucose on intraperitoneal administration at 10 mg/kg, ...