title: Discovery of DA-1229: a potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes.
abstract: A series of β-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)-piperazin-2-one (DA-1229) displayed potent DPP-4 inhibition pattern in several animal models, was selected for clinical development.
authors.affiliation: Dong-A Pharm. Co., Ltd, Yongin-si, Gyeonggi-do, Republic of Korea.
authors.forename: Heung Jae
authors.initials: HJ
authors.lastname: Kim
authors.forename: Woo Young
authors.initials: WY
authors.lastname: Kwak
authors.forename: Jong Pil
authors.initials: JP
authors.lastname: Min
authors.forename: Jae Young
authors.initials: JY
authors.lastname: Lee
authors.forename: Tae Hyun
authors.initials: TH
authors.lastname: Yoon
authors.forename: Ha Dong
authors.initials: HD
authors.lastname: Kim
authors.forename: Chang Yell
authors.initials: CY
authors.lastname: Shin
authors.forename: Mi Kyung
authors.initials: MK
authors.lastname: Kim
authors.forename: Song Hyen
authors.initials: SH
authors.lastname: Choi
authors.forename: Hae Sun
authors.initials: HS
authors.lastname: Kim
authors.forename: Eun Kyoung
authors.initials: EK
authors.lastname: Yang
authors.forename: Ye Hwang
authors.initials: YH
authors.lastname: Cheong
authors.forename: Yu Na
authors.initials: YN
authors.lastname: Chae
authors.forename: Kyung Jin
authors.initials: KJ
authors.lastname: Park
authors.forename: Ji Myun
authors.initials: JM
authors.lastname: Jang
authors.forename: Soo Jung
authors.initials: SJ
authors.lastname: Choi
authors.forename: Moon Ho
authors.initials: MH
authors.lastname: Son
authors.forename: Soon Hoe
authors.initials: SH
authors.lastname: Kim
authors.forename: Moohi
authors.initials: M
authors.lastname: Yoo
authors.forename: Bong Jin
authors.initials: BJ
authors.lastname: Lee
mesh_terms: D000284:Administration, Oral; D000818:Animals; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004195:Disease Models, Animal; D006801:Humans; D020128:Inhibitory Concentration 50; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: C557982:4-(3-amino-4-(2,4,5-trifluorophenyl)butanoyl)-3-(tert-butoxymethyl)piperazin-2-one; D054873:Dipeptidyl-Peptidase IV Inhibitors; D010879:Piperazines