Abstract
A series of benzothiazinone and benzooxazinone derivatives were discovered as SGLT2 inhibitors. The optimization led to the discovery of compounds 31 and 32, which exhibited similar potency and better SGLT1 selectivity compared to dapagliflozin. These compounds may provide novel promising scaffolds, which are different from phlorizin-based SGLT2 inhibitors.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Benzoxazines / chemical synthesis
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Benzoxazines / chemistry*
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Benzoxazines / pharmacology
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Drug Evaluation, Preclinical
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Humans
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Mice
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Rats
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Sodium-Glucose Transporter 1 / antagonists & inhibitors
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Sodium-Glucose Transporter 1 / metabolism
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Sodium-Glucose Transporter 2 / metabolism
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Sodium-Glucose Transporter 2 Inhibitors*
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Thiazines / chemical synthesis
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Thiazines / chemistry
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Thiazines / pharmacology
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Triazoles / chemical synthesis
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Triazoles / chemistry*
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Triazoles / pharmacology
Substances
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Benzoxazines
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Sodium-Glucose Transporter 1
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Sodium-Glucose Transporter 2
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Sodium-Glucose Transporter 2 Inhibitors
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Thiazines
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Triazoles