57690-96-7Relevant articles and documents
Discovery of potent, low-absorbable sodium-dependent glucose cotransporter 1 (SGLT1) inhibitor SGL5213 for type 2 diabetes treatment
Kuroda, Shoichi,Kobashi, Yohei,Oi, Takahiro,Kawabe, Kenichi,Shiozawa, Fumiyasu,Okumura-Kitajima, Lisa,Sugisaki-Kitano, Mami,Io, Fusayo,Yamamoto, Koji,Kakinuma, Hiroyuki
, p. 394 - 409 (2019/01/04)
A new series of C-phenyl D-glucitol derivatives was designed and synthesized, and their SGLT1 inhibitory potency and absorbability were evaluated. We also investigated whether kidney drug retention could be avoided by creating molecules with different excretion pathways. To achieve a class of molecules with low absorption and that were excreted in bile, optimized synthesis was performed to bring the ClogP value and the topological polar surface area to within the appropriate ranges. Compounds 34d and 34j were poorly absorbed, but the absorbed compounds were mainly excreted in bile. Thus, smaller amounts of persistent residue in the kidneys were observed. Since 34d exerted a glucose-lowering effect at a dose of 0.3 mg/kg (p.o.) in SD rats, this compound (SGL5213) could be a clinical candidate for the treatment of type 2 diabetes.
4-ISOPROPYL-6-METHOXYPHENYL GLUCITOL COMPOUND
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Paragraph 0149; 0150; 0151; 0152; 0153, (2013/07/05)
A compound, which inhibits SGLT1 (sodium-dependent glucose transporter 1) activity to suppress absorption of glucose or the like, thereby suppressing abnormal glucose tolerance or postprandial hyperglycemia in diabetes, is provided. Specifically, a 4-isopropyl-6-methoxyphenyl glucitol compound represented by the following formula (I), or a pharmaceutically acceptable salt thereof, is provided:
Neutral nazarov-type cyclization catalyzed by palladium(0)
Shimada, Naoyuki,Stewart, Craig,Bow, William F.,Jolit, Anais,Wong, Kahoano,Zhou, Zhe,Tius, Marcus A.
supporting information; experimental part, p. 5727 - 5729 (2012/08/07)
Joining the circle: The first Pd0 catalyzed Nazarov-type cyclization of diketoesters (see scheme) proceeds in 70 % to 95 % yield under strictly neutral pH conditions. Aryl substitution of the diketoesters is not required, so the reaction shows great versatility and can also proceed with aliphatic substrates. Copyright