| Title : Discovery of DA-1229: a potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes - Kim_2011_Bioorg.Med.Chem.Lett_21_3809 |
| Author(s) : Kim HJ , Kwak WY , Min JP , Lee JY , Yoon TH , Kim HD , Shin CY , Kim MK , Choi SH , Kim HS , Yang EK , Cheong YH , Chae YN , Park KJ , Jang JM , Choi SJ , Son MH , Kim SH , Yoo M , Lee BJ |
| Ref : Bioorganic & Medicinal Chemistry Lett , 21 :3809 , 2011 |
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Abstract :
A series of beta-amino amide containing substituted piperazine-2-one derivatives was synthesized and evaluated as inhibitors of dipeptidyl pepdidase-4 (DPP-4) for the treatment of type 2 diabetes. As results of intensive SAR study of the series, (R)-4-[(R)-3-amino-4-(2,4,5-trifluorophenyl)-butanoyl]-3-(t-butoxymethyl)-piperaz in-2-one (DA-1229) displayed potent DPP-4 inhibition pattern in several animal models, was selected for clinical development. |
| PubMedSearch : Kim_2011_Bioorg.Med.Chem.Lett_21_3809 |
| PubMedID: 21570283 |
Kim HJ, Kwak WY, Min JP, Lee JY, Yoon TH, Kim HD, Shin CY, Kim MK, Choi SH, Kim HS, Yang EK, Cheong YH, Chae YN, Park KJ, Jang JM, Choi SJ, Son MH, Kim SH, Yoo M, Lee BJ (2011)
Discovery of DA-1229: a potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes
Bioorganic & Medicinal Chemistry Lett
21 :3809
Kim HJ, Kwak WY, Min JP, Lee JY, Yoon TH, Kim HD, Shin CY, Kim MK, Choi SH, Kim HS, Yang EK, Cheong YH, Chae YN, Park KJ, Jang JM, Choi SJ, Son MH, Kim SH, Yoo M, Lee BJ (2011)
Bioorganic & Medicinal Chemistry Lett
21 :3809