Design and synthesis of new potent dipeptidyl peptidase IV inhibitors with enhanced ex vivo duration

被引：18

作者：

Kondo, Takashi ^{[1
]}

Nekado, Takahiro ^{[1
]}

Sugimoto, Isamu ^{[1
]}

Ochi, Kenya ^{[1
]}

Takai, Shigeyuki ^{[1
]}

Kinoshita, Atsushi ^{[1
]}

Tajima, Yohei ^{[1
]}

Yamamoto, Susumu ^{[1
]}

Kawabata, Kazuhito ^{[1
]}

Nakai, Hisao ^{[1
]}

Toda, Masaaki ^{[1
]}

机构：

[1] Ono Pharmaceut Co Ltd, Minase Res Inst, Osaka 6188585, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 07期

关键词：

DPP-IV inhibitor; protyl-2-cyanopyrrolidine;

D O I：

10.1016/j.bmc.2007.01.041

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of 5 beta-methylprolyl-2-cyanopyrrolidine analogs were synthesized and evaluated as DPP-IV inhibitors, and the duration of their ex vivo activity was assessed. Comparison of their potency and duration of action was done among three different species. The mode of binding was investigated, and the effect on the plasma glucose level was evaluated. Structure-activity relationships are also presented. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：2631 / 2650

页数：20

共 24 条

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[23] Scaffold-based design of xanthine as highly potent inhibitors of DPP-IV for improving glucose homeostasis in DIO mice
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