Synthesis and evaluation of camphor and cytisine-based cyanopyrrolidines as DPP-IV inhibitors for the treatment of type 2 diabetes mellitus

被引：28

作者：

Kuranov, S. O. ^{[1
]}

Tsypysheva, I. P. ^{[2
]}

Khvostov, M., V ^{[1
,5
]}

Zainullina, Liana F. ^{[3
,4
]}

Borisevich, S. S. ^{[2
]}

Vakhitova, Yu V. ^{[3
,4
]}

Luzina, O. A. ^{[1
]}

Salakhutdinov, N. F. ^{[1
,5
]}

机构：

[1] Russian Acad Sci, Siberian Branch, NN Vorozhtsov Novosibirsk Inst Organ Chem, Novosibirsk 630090, Russia

[2] Russian Acad Sci, Ufa Inst Chem, Ufa 450054, Russia

[3] FSBI Zalcusov Inst Pharmacol, Moscow 125315, Russia

[4] IBG UFRC RAS, Ufa 450054, Russia

[5] Novosibirsk State Univ, Novosibirsk 630090, Russia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2018年 / 26卷 / 15期

关键词：

DIPEPTIDYL-PEPTIDASE-IV; COMPLICATIONS; EPIDEMIOLOGY; DERIVATIVES; INSULIN; DESIGN; POTENT; DRUGS;

D O I：

10.1016/j.bmc.2018.07.018

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：

In this study, bornyl- and cytisine-based cyanopyrrolidines as potent dipeptidyl peptidase-IV (DPP-IV) inhibitors were synthesised. The in vitro inhibiting activities of bornyl- and cytisine derivatives towards DPP-IV were evaluated. Bornyl-based cyanopyrrolidines were shown to have moderate inhibitory activity with regard to DPP-IV (1.27-15.78 mu M). A docking study was performed to elucidate the structure-activity relationship of the obtained compounds. The in vivo hypoglycemic activities of the same compounds were evaluated with the oral glucose tolerance test (OGTT) in mice. Bornyl-based cyanopyrrolidines were shown to have good hypoglycemic activity.

引用

页码：4402 / 4409

页数：8

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