Synthesis and biological activity of some new flavonyl-2,4-thiazolidinediones

被引：44

作者：

Bozdag-Duendar, Oya ^{[1
]}

Verspohl, Eugen J. ^{[2
]}

Das-Evcimen, Net ^{[3
]}

Kaup, Rebecca M. ^{[2
]}

Bauer, Katrin ^{[2
]}

Sarikaya, Mutlu ^{[3
]}

Evranos, Beguem ^{[1
]}

Ertan, Rahmiye ^{[1
]}

机构：

[1] Ankara Univ, Dept Pharmaceut Chem, Fac Pharm, TR-06100 Ankara, Turkey

[2] Univ Munster, Inst Med Chem, Dept Pharmacol, Munster, Germany

[3] Ankara Univ, Fac Pharm, Dept Biochem, TR-06100 Ankara, Turkey

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2008年 / 16卷 / 14期

关键词：

antidiabetic agents; flavone; 2,4-thiazolidinediones; flavonyl-2,4-thiazolidinediones; insulinotropic activity; aldose reductase inhibition; synthesis;

D O I：

10.1016/j.bmc.2008.05.059

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 new series of flavonyl-2,4-thiazolidinediones (Va-c, VIa-c) was prepared by Knoevenagel reaction. The synthesized compounds were tested for their ability to inhibit rat kidney aldose reductase (AR) and for their insulinotropic activities in INS-1 cells. Compound Vb was able to increase insulin release in the presence of 5.6 mmol/l glucose. Compounds VIa-c displayed moderate to high AR inhibitory activity levels. Particularly, compound VIa showed the highest AR inhibitory activity (86.57%). (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：6747 / 6751

页数：5

共 39 条

[1] ESTABLISHMENT OF 2-MERCAPTOETHANOL-DEPENDENT DIFFERENTIATED INSULIN-SECRETING CELL-LINES [J].

ASFARI, M ;

JANJIC, D ;

MEDA, P ;

LI, GD ;

HALBAN, PA ;

WOLLHEIM, CB .

ENDOCRINOLOGY, 1992, 130 (01) :167-178

[2]

Bozdag O, 2000, ARZNEIMITTELFORSCH, V50, P626

[3]

Bozdag O, 2000, ARZNEIMITTELFORSCH, V50, P539

[4]

Bozdag O, 1999, ARCH PHARM, V332, P435, DOI 10.1002/(SICI)1521-4184(199912)332:12<435::AID-ARDP435>3.0.CO

[5]

2-L

[6]

Bozdag-Dündar O, 2001, ARZNEIMITTEL-FORSCH, V51, P623

[7]

BRADFORD MM, 1976, ANAL BIOCHEM, V72, P248, DOI 10.1016/0003-2697(76)90527-3

[8] Aldose reductase inhibitor zopolrestat restores allergic hyporesponsiveness in alloxan-diabetic rats [J].

Carvalho, Vinicius F. ;

Barreto, Emiliano O. ;

Serra, Magda F. ;

Cordeiro, Renato S. B. ;

Martins, Marco A. ;

Fortes, Zuleica Bruno ;

Silva, Patricia M. R. e .

EUROPEAN JOURNAL OF PHARMACOLOGY, 2006, 549 (1-3) :173-178

[9] ANTIINFLAMMATORY AND ALDOSE REDUCTASE INHIBITORY ACTIVITY OF SOME TRICYCLIC ARYLACETIC ACIDS [J].

CERELLI, MJ ;

CURTIS, DL ;

DUNN, JP ;

NELSON, PH ;

PEAK, TM ;

WATERBURY, LD .

JOURNAL OF MEDICINAL CHEMISTRY, 1986, 29 (11) :2347-2351

[10] Pharmacological approaches to the treatment of diabetic complications [J].

Costantino, L ;

Rastelli, G ;

Gamberini, MC ;

Barlocco, D .

EXPERT OPINION ON THERAPEUTIC PATENTS, 2000, 10 (08) :1245-1262

← 1 2 3 4 →