842133-87-3

Upstream product

• 1450738-12-1 2-(5-bromo-2-methylbenzyl)-5-chlorothiophene 
• 1450738-11-0 (5-bromo-2-methylphenyl)(5-chlorothiophen-2-yl)methanone 
• 79669-49-1 5-bromo-2-methylbenzoic acid 
• 842132-58-5 3-[(5-chloro-2-thienyl)methyl]-1-(β-D-glucopyranosyl)-4-methylbenzene 
• 108-24-7 acetic anhydride 
• 21900-41-4 5-bromo-2-methylbenzoyl?chloride 

Downstream Products

• 842133-96-4 4-methyl-1-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl)-3-[(5-(5-pyrimidyl)-2-thienyl)methyl]benzene 
• 866607-37-6 4-methyl-1-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl)-3-[(5-(2-pyrimidyl)-2-thienyl)methyl]benzene 
• 1450738-10-9 4-methyl-1-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl)-3-[(5-(5-thiazolyl)-2-thienyl)methyl]benzene 
• 842134-42-3 1-(β-D-glucopyranosyl)-4-methyl-3-[(5-(2-pyrimidyl)-2-thienyl)methyl]benzene 
• 842134-89-8 1-(β-D-glucopyranosyl)-4-methyl-3-[(5-(5-thiazolyl)-2-thienyl)methyl]benzene 
• 842134-31-0 4-methyl-1-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl)-3-[2-thienylmethyl]benzene 
• 842134-33-2 3-[(5-bromo-2-thienyl)methyl]-4-methyl-1-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl)benzene 

Relevant academic research and scientific papers

C-Glucosides with heteroaryl thiophene as novel sodium-dependent glucose cotransporter 2 inhibitors

Canagliflozin (1), a novel inhibitor for sodium-dependent glucose cotransporter 2 (SGLT2), has been developed for the treatment of type 2 diabetes. To investigate the effect of replacement of the phenyl ring in 1 with heteroaromatics, C-glucosides 2 were designed, synthesized, and evaluated for their inhibitory activities against SGLT2. Of these, 3-pyridyl, 2-pyrimidyl or 5-membered heteroaryl substituted derivatives showed highly potent inhibitory activity against SGLT2, while 5-pyrimidyl substitution was associated with slightly reduced activity. In particular, 2g (TA-3404) had remarkable anti-hyperglycemic effects in high-fat diet fed KK (HF-KK) mice.