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, synthesis and antiproliferative activity of tripentones: A new series of antitubulin agents
Lisowski, Vincent,Enguehard, Cecile,Lancelot, Jean-Charles,Caignard, Daniel-Henri,Lambel, Stephanie,Leonce, Stephane,Pierre, Alain,Atassi, Ghanem,Renard, Pierre,Rault, Sylvain
, p. 2205 - 2208 (2007/10/03)
Structure-activity relationship studies of a new series of tripentones (thieno[2,3-b]pyrrolizin-8-ones), led us to prepare several derivatives with antiproliferative activities. The most promising 3-(3-hydroxy-4-methoxyphenyl)thieno[2,3-b]pyrrolizin-8-one 20 (leukemia L1210, IC50 = 15 nM) was shown to be a potent inhibitor of tubulin polymerization.
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.
Analgetic compounds, compositions and process of treatment
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, (2008/06/13)
Novel compounds of the formula: STR1 wherein R1 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, CH2 -alkenyl wherein alkenyl is from 2 to 4 carbon atoms, inclusive, cycloalkyl of from 3 to 6 carbon atoms, inclusive, cycloalkylmethyl of from 3 to 6 carbon atoms, inclusive; R2 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, inclusive, with the proviso that R1 and R2 cannot both be hydrogen at the same time; Y is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive, halogen, trifluoromethyl, hydroxy, alkanoyloxy from 2 to 5 carbon atoms, inclusive, alkoxy of from 1 to 4 carbon atoms, inclusive, cycloalkyloxy of from 3 to 6 carbon atoms, inclusive, benzyloxy; m is an integer 0, 1, 2; R5 is a variable consisting of hydrogen and alkyl of from 1 to 4 carbon atoms, inclusive; R3 is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive; R4 is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive, CH2 -alkenyl wherein alkenyl is of from 2 to 4 carbon atoms, inclusive, and arylalkyl wherein alkyl is from 1 to 4 carbon atoms, inclusive, and aryl is STR2 WHEREIN Y' is CF3, halogen, alkyl of 1 to 4 carbon atoms, inclusive, and alkoxy of from 1 to 4 carbon atoms, inclusive; and R3 and R4 when taken together with the nitrogen atom to which they are attached can form saturated heterocycles of from 5 to 7 ring members, a second hetero atom of said ring can be oxygen or nitrogen, e.g., morpholine, piperazine, and said heterocycles can be monosubstituted having a total of up to 9 carbon atoms, with the proviso that when STR3 is pyrrolidinyl, then m = 1, 2, having analgetic activity in humans and animals are prepared in unit dosage forms. The compositions are useful in relieving pain by administering orally, parenterally, and rectally to humans and animals.
