Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents

被引：41

作者：

Datar, Prasanna A. ^{[1
]}

Jadhav, Sonali R. ^{[1
]}

机构：

[1] Sinhgad Inst Pharm, Dept Pharmaceut Chem, Pune 411041, Maharashtra, India

来源：

INTERNATIONAL JOURNAL OF MEDICINAL CHEMISTRY | 2015年 / 2015卷

关键词：

D O I：

10.1155/2015/670181

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Pyrazole-3-one compounds were designed on the basis of docking studies of previously reported antidiabetic pyrazole compounds. The amino acid residues found during docking studies were used as guidelines for the modification of aromatic substitutions on pyrazole-3-one structure. Depending on the docking score, the designed compounds were selectively prioritized for synthesis. The synthesized compounds were subjected to in vivo hypoglycemic activity using alloxan induced diabetic rats and metformin as a standard. Compound 4 having sulphonamide derivative was found to be the most potent compound among the series.

引用

页数：10

共 22 条

[1] Synthesis of novel pyrazole derivatives and evaluation of their antidepressant and anticonvulsant activities [J].

Abdel-Aziz, Mohamed ;

Abuo-Rahma, Gamal El-Din A. ;

Hassan, Alaa A. .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (09) :3480-3487

[2]

Adeghate Ernest, 2011, Open Med Chem J, V5, P68, DOI 10.2174/1874104501105010068

[3]

Akinola O, 2012, OPEN DIABETES J, V5, P8, DOI [DOI 10.2174/1876524601205010008, 10.2174/1876524601205010008]

[4]

Alam MM, 2013, ACTA POL PHARM, V70, P435

[5] The pharmacology of diabetic complications [J].

Altan, VM .

CURRENT MEDICINAL CHEMISTRY, 2003, 10 (15) :1317-1327

[6] Metabolic effects of two years of exenatide treatment on diabetes, obesity, and hepatic biomarkers in patients with type 2 diabetes: An interim analysis of data from the open-label, uncontrolled extension of three double-blind, placebo-controlled trials [J].

Buse, John B. ;

Klonoff, David C. ;

Nielsen, Loretta L. ;

Guan, Xuesong ;

Bowlus, Christopher L. ;

Holcombe, John H. ;

Maggs, David G. ;

Wintle, Matthew E. .

CLINICAL THERAPEUTICS, 2007, 29 (01) :139-153

[7] Synthesis and hypoglycemic evaluation of substituted pyrazole-4-carboxylic acids [J].

Cottineau, B ;

Toto, P ;

Marot, C ;

Pipaud, A ;

Chenault, J .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (16) :2105-2108

[8]

Das N, 2008, INDIAN J CHEM B, V47, P1555

[9] Synthesis and antiviral activity of new pyrazole and thiazole derivatives [J].

El-Sabbagh, Osama I. ;

Baraka, Mohamed M. ;

Ibrahim, Samy M. ;

Pannecouque, Christophe ;

Andrei, Graciela ;

Snoeck, Robert ;

Balzarini, Jan ;

Rashad, Adel A. .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (09) :3746-3753

[10] Synthesis and biological evaluation of new 3-trifluoromethylpyrazolesulfonyl-urea and thiourea derivatives as antidiabetic and antimicrobial agents [J].

Faidallah, Hassan M. ;

Khan, Khalid A. ;

Asiri, Abdullah M. .

JOURNAL OF FLUORINE CHEMISTRY, 2011, 132 (02) :131-137

← 1 2 3 →