852631-01-7Relevant academic research and scientific papers
Design and synthesis of a monocyclic derivative as a selective ACC1 inhibitor by chemical modification of biphenyl ACC1/2 dual inhibitors
Mizojiri, Ryo,Tomita, Daisuke,Sasaki, Masako,Satoh, Yoshihiko,Yamamoto, Yukiko,Sumi, Hiroyuki,Maezaki, Hironobu
, (2021/02/26)
A structure–activity relationship (SAR) study towards novel ACC1-selective inhibitors was carried out by modifying the molecular length of the linker in biaryl derivative 1 g, an ACC1/2 dual inhibitor. Ultimately, this leads us to discover novel phenoxybenzyloxy derivative 1i as a potent ACC1-selective inhibitor. Further chemical modification of this scaffold to improve cellular potency as well as physicochemical and pharmacokinetic (PK) properties produced N-2-(pyridin-2-ylethyl)acetamide derivative 1n, which showed highly potent ACC1-selective inhibition as well as sufficient PK profile for further in vivo evaluations. Oral administration of 1n significantly reduced the concentration of malonyl-CoA in HCT-116 xenograft tumors at doses of 100 mg/kg. Accordingly, our novel series of potent ACC1-selective inhibitors represents a set of useful orally-available research tools, as well as potential therapeutic agents for cancer and fatty acid-related diseases.
NOVEL SGLT INHIBITORS
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Paragraph 0174, (2017/06/23)
The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synt
NOVEL SGLT INHIBITORS
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Page/Page column 73, (2013/03/28)
The present invention relates to novel compounds of Formula (I), their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the sy
C-5-disubstituted barbiturates as potential molecular probes for noninvasive matrix metalloproteinase imaging
Breyholz, Hans-J?rg,Sch?fers, Michael,Wagner, Stefan,H?ltke, Carsten,Faust, Andreas,Rabeneck, Helmut,Levkau, Bodo,Schober, Otmar,Kopka, Klaus
, p. 3400 - 3409 (2007/10/03)
Studies have demonstrated a positive correlation between inflammation, metastasis, or atherosclerosis and the unbalanced or culminated expression of matrix metalloproteinases (MMPs). The molecular imaging of locally upregulated MMP activity in vivo is a c
