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Your search keyword '"Nakabayashi, Takeshi"' showing total 1 results
Start Over Author "Nakabayashi, Takeshi" Topic chemical derivatives
1 results on '"Nakabayashi, Takeshi"'

1. Structure–activity relationship studies of 4-benzyl-1H-pyrazol-3-yl β-d-glucopyranoside derivatives as potent and selective sodium glucose co-transporter 1 (SGLT1) inhibitors with therapeutic activity on postprandial hyperglycemia

Author

Fushimi, Nobuhiko, Fujikura, Hideki, Shiohara, Hiroaki, Teranishi, Hirotaka, Shimizu, Kazuo, Yonekubo, Shigeru, Ohno, Kohsuke, Miyagi, Takashi, Itoh, Fumiaki, Shibazaki, Toshihide, Tomae, Masaki, Ishikawa-Takemura, Yukiko, Nakabayashi, Takeshi, Kamada, Noboru, Ozawa, Tomonaga, Kobayashi, Susumu, and Isaji, Masayuki

Subjects
*BENZYL group, *HETEROCYCLIC compounds synthesis, *PYRAZOLES, *GLUCOPYRANOSIDE, *CHEMICAL derivatives, *SODIUM compounds, *HYPERGLYCEMIA treatment, *NICOTINAMIDE, *STREPTOZOTOCIN
Abstract

Abstract: Sodium glucose co-transporter 1 (SGLT1) plays a dominant role in the absorption of glucose in the gut and is considered a promising target in the development of treatments for postprandial hyperglycemia. A series of 4-benzyl-1H-pyrazol-3-yl β-d-glucopyranoside derivatives have been synthesized, and its inhibitory activity toward SGLTs has been evaluated. By altering the substitution groups at the 5-position of the pyrazole ring, and every position of the phenyl ring, we studied the structure–activity relationship (SAR) profiles and identified a series of potent and selective SGLT1 inhibitors. Representative derivatives showed a dose-dependent suppressing effect on the escalation of blood glucose levels in oral mixed carbohydrate tolerance tests (OCTT) in streptozotocin–nicotinamide-induced diabetic rats (NA-STZ rats). [Copyright &y& Elsevier]

Published
2012
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