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; Isaji, Masayuki published the artcile< 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>, SDS of cas: 112-63-0, the main research area is preparation structure benzyl pyrazolyl glucopyranoside derivative SGLT1 inhibitor hyperglycemia.
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 Ph 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).
Bioorganic & Medicinal Chemistry published new progress about Antidiabetic agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, SDS of cas: 112-63-0.
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