Pyrazolidine derivatives with heteroaryl urea as dipeptidyl peptidase IV inhibitors

被引：16

作者：

Ahn, JH ^{[1
]}

Jung, SH

Kim, JA

Song, SB

Kwon, SJ

Kim, KR

Dal Rhee, S

Park, SD

Lee, JM

Kim, SS

Cheon, HG

机构：

[1] Korea Res Inst Chem Technol, Div Med Sci, Taejon 305600, South Korea

[2] JEIL Pharmaceut Co Ltd, R&D Ctr, Yongin 449861, South Korea

[3] CJ Corp, R&D Ctr Pharmaceut, Ichon 467810, South Korea

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2005年 / 53卷 / 08期

关键词：

dipeptidyl peptidase IV (DP-IV); pyrazolidine; anti-diabetic agent;

D O I：

10.1248/cpb.53.1048

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In the continuation of efforts to modify the structure of our novel DP-IV inhibitors, a series of pyrazolidine derivatives with heteroaryl urea was synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV).

引用

页码：1048 / 1050

页数：3

共 19 条

[1] Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors [J].

Ahn, JH ;

Kim, JA ;

Kim, HM ;

Kwon, HM ;

Huh, SC ;

Rhee, SD ;

Kim, KR ;

Yang, SD ;

Park, SD ;

Lee, JM ;

Kim, SS ;

Cheon, HG .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (05) :1337-1340

[2] Synthesis and DP-IV inhibition of cyano-pyrazoline derivatives as potent anti-diabetic agents [J].

Ahn, JH ;

Kim, HM ;

Jung, SH ;

Kang, SK ;

Kim, KR ;

Rhee, SD ;

Yang, SD ;

Cheon, HG ;

Kim, SS .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2004, 14 (17) :4461-4465

[3] Diastereoselective synthesis and configuration-dependent activity of (3-substituted-cycloalkyl)glycine pyrrolidides and thiazolidides as dipeptidyl peptidase IV inhibitors [J].

Ashton, WT ;

Dong, H ;

Sisco, RM ;

Doss, GA ;

Leiting, B ;

Patel, RA ;

Wu, JK ;

Marsilio, F ;

Thornberry, NA ;

Weber, AE .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2004, 14 (04) :859-863

[4] Inhibition of dipeptidyl peptidase IV with NVP-DPP728 increases plasma GLP-1 (7-36 amide) concentrations and improves oral glucose tolerance in obese Zucker rats [J].

Balkan, B ;

Kwasnik, L ;

Miserendino, R ;

Holst, JJ ;

Li, X .

DIABETOLOGIA, 1999, 42 (11) :1324-1331

[5] Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors [J].

Caldwell, CG ;

Chen, P ;

He, JF ;

Parmee, ER ;

Leiting, B ;

Marsilio, F ;

Patel, RA ;

Wu, JK ;

Eiermann, GJ ;

Petrov, A ;

He, HB ;

Lyons, KA ;

Thornberry, NA ;

Weber, AE .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2004, 14 (05) :1265-1268

[6] Dipeptidyl peptidase IV inhibition potentiates the insulinotropic effect of glucagon-like peptide 1 in the anesthetized pig [J].

Deacon, CF ;

Hughes, TE ;

Holst, JJ .

DIABETES, 1998, 47 (05) :764-769

[7] Glucagon-like peptides [J].

Drucker, DJ .

DIABETES, 1998, 47 (02) :159-169

[8] DEGRADATION OF GLUCOSE-DEPENDENT INSULINOTROPIC POLYPEPTIDE AND TRUNCATED GLUCAGON-LIKE PEPTIDE-1 IN-VITRO AND IN-VIVO BY DIPEPTIDYL PEPTIDASE-IV [J].

KIEFFER, TJ ;

MCINTOSH, CHS ;

PEDERSON, RA .

ENDOCRINOLOGY, 1995, 136 (08) :3585-3596

[9] (2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-α]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine:: A potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes [J].

Kim, D ;

Wang, LP ;

Beconi, M ;

Eiermann, GJ ;

Fisher, MH ;

He, HB ;

Hickey, GJ ;

Kowalchick, JE ;

Leiting, B ;

Lyons, K ;

Marsilio, F ;

McCann, ME ;

Patel, RA ;

Petrov, A ;

Scapin, G ;

Patel, SB ;

Roy, RS ;

Wu, JK ;

Wyvratt, MJ ;

Zhang, BB ;

Zhu, L ;

Thornberry, NA ;

Weber, AE .

JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (01) :141-151

[10] Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability:: Interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of α-aminoacyl-L-cis-4,5-methanoprolinenitrile-based inhibitors [J].

Magnin, DR ;

Robl, JA ;

Sulsky, RB ;

Augeri, DJ ;

Huang, YT ;

Simpkins, LM ;

Taunk, PC ;

Betebenner, DA ;

Robertson, JG ;

Abboa-Offei, BE ;

Wang, AY ;

Cap, M ;

Xin, L ;

Tao, L ;

Sitkoff, DF ;

Malley, MF ;

Gougoutas, JZ ;

Khanna, A ;

Huang, Q ;

Han, SP ;

Parker, RA ;

Hamann, LG .

JOURNAL OF MEDICINAL CHEMISTRY, 2004, 47 (10) :2587-2598

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