| Title : Synthesis and potent inhibitory activities of carboxybenzyl-substituted 8-(3-(R)-aminopiperidin-1-yl)-7-(2-chloro\/cyanobenzyl)-3-methyl-3,7-dihydro-purin e-2,6-diones as dipeptidyl peptidase IV (DPP-IV) inhibitors - Mo_2015_Bioorg.Med.Chem.Lett_25_1872 |
| Author(s) : Mo DW , Dong S , Sun H , Chen JS , Pang JX , Xi BM , Chen WH |
| Ref : Bioorganic & Medicinal Chemistry Lett , 25 :1872 , 2015 |
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Abstract :
Fourteen 3-methyl-3,7-dihydro-purine-2,6-dione derivatives 1-14 bearing carboxybenzyl and 2-chloro/cyanobenzyl groups at the N-1 and N-7 positions, respectively, were synthesized as dipeptidyl peptidase IV (DPP-IV) inhibitors. These compounds were characterized on the basis of NMR ((1)H and (13)C) and ESI MS data. In vitro bioassay indicates that most of these compounds showed moderate to good inhibitory activities against DPP-IV. Among them, compound 13 (IC50=36nM) exhibited comparable activity with a positive control, Sitagliptin (IC50=16nM). In addition, the structure-activity relationship of these compounds is also briefly discussed. |
| PubMedSearch : Mo_2015_Bioorg.Med.Chem.Lett_25_1872 |
| PubMedID: 25838146 |
Mo DW, Dong S, Sun H, Chen JS, Pang JX, Xi BM, Chen WH (2015)
Synthesis and potent inhibitory activities of carboxybenzyl-substituted 8-(3-(R)-aminopiperidin-1-yl)-7-(2-chloro\/cyanobenzyl)-3-methyl-3,7-dihydro-purin e-2,6-diones as dipeptidyl peptidase IV (DPP-IV) inhibitors
Bioorganic & Medicinal Chemistry Lett
25 :1872
Mo DW, Dong S, Sun H, Chen JS, Pang JX, Xi BM, Chen WH (2015)
Bioorganic & Medicinal Chemistry Lett
25 :1872