6775-77-5Relevant articles and documents
Design, synthesis and in vivo hypoglycemic activity of tetrazole-bearing N-glycosides as SGLT2 inhibitors
Gao,Zhao,Liu,Shao,Wang,Tang,Wang
experimental part, p. 1499 - 1508 (2011/02/22)
Novel tetrazole-bearing N-glycosides have been designed and synthesized as SGLT2 inhibitors via a conventional protocol starting from substituted phenylacetic acids and two monosaccharides, D-glucose and D-galactose, and their hypoglycemic activity has been tested in vivo by mice oral glucose tolerance test (OGTT). Two compounds are found to be more potent than the positive control Dapagliflozin. The structure-activity relationship has also been investigated.
Design of Inhibitors from the Three-Dimensional Structure of Alcohol Dehydrogenase. Chemical Synthesis and Enzymatic Properties
Freudenreich, Charles,Samama, Jean-Pierre,Biellmann, Jean-Francois
, p. 3344 - 3353 (2007/10/02)
Inhibitors of liver alcohol dehydrogenase were designed from the three-dimensional structure of the enzyme.The ligand to the catalytic zinc ion is an amide group or, better, a formamide group.With the latter function, a hydrogen bond between the NH group and the hydroxyl group of Ser-48 may be formed.The hydrophobic substrate binding site brings structural restraints. α-ω bifunctional molecules show good inhibitory properties possibly due to the interactions with polar residues at the entrance of the substrate binding site.
