Literature DB >> 21570283

Discovery of DA-1229: a potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes.

Heung Jae Kim1, Woo Young Kwak, Jong Pil Min, Jae Young Lee, Tae Hyun Yoon, Ha Dong Kim, Chang Yell Shin, Mi Kyung Kim, Song Hyen Choi, Hae Sun Kim, Eun Kyoung Yang, Ye Hwang Cheong, Yu Na Chae, Kyung Jin Park, Ji Myun Jang, Soo Jung Choi, Moon Ho Son, Soon Hoe Kim, Moohi Yoo, Bong Jin Lee.   

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.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21570283     DOI： 10.1016/j.bmcl.2011.04.029

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

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2.  DA-1229, a dipeptidyl peptidase IV inhibitor, protects against renal injury by preventing podocyte damage in an animal model of progressive renal injury.

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6.  Multiple-dose pharmacokinetics and pharmacodynamics of evogliptin (DA-1229), a novel dipeptidyl peptidase IV inhibitor, in healthy volunteers.

Authors:  Namyi Gu; Min Kyu Park; Tae-Eun Kim; Mi Young Bahng; Kyoung Soo Lim; Sang-Heon Cho; Seo Hyun Yoon; Joo-Youn Cho; In-Jin Jang; Kyung-Sang Yu
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Authors:  Yu-Na Chae; Tae-Hyoung Kim; Mi-Kyung Kim; Chang-Yell Shin; Il-Hoon Jung; Yong Sung Sohn; Moon-Ho Son
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Authors:  Su-Jin Rhee; YoonJung Choi; SeungHwan Lee; Jaeseong Oh; Sung-Jin Kim; Seo Hyun Yoon; Joo-Youn Cho; Kyung-Sang Yu
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  9 in total

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