DPPH Scavenging Assay of Novel 1,3-disubstituted-1H-pyrazol-5-ols and their in silico Studies on Some Proteins Involved in Alzheimer's Disease Signaling Cascade

被引：36

作者：

Sarojini, Balladka Kunhanna ^{[1
]}

Vidyagayatri, Marakkur ^{[1
,2
]}

Darshanraj, Chenna Govindaraju ^{[1
]}

Bharath, Basavapattana Rudresh ^{[3
]}

Manjunatha, Hanumanthappa ^{[3
]}

机构：

[1] PA Coll Engn, Dept Chem, Mangalore 574153, Karnataka, India

[2] Syngine Int Ltd, SUO13, Bangalore 99, Karnataka, India

[3] Kuvempu Univ, Dept PG Studies & Res Biotechnol & Bioinformat, Shankaraghatta 577451, Karnataka, India

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2010年 / 7卷 / 03期

关键词：

AD; Pyrazole derivative; DPPH assay; Molecular docking studies; GSK-3; beta; beta-secretase; INHIBITION;

D O I：

10.2174/157018010790596588

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of new 1,3-disubstituted-1H-pyrazol-5-ols (3) which are the analogues of known radical scavenger 'edaravone' are synthesized, characterized and evaluated for DPPH scavenging capacity. The docking studies are carried out for these compounds in the enol form and also in the respective keto form against the proteins and peptides involved in Alzhemier disease signal cascade. Some of them showed good radical scavenging capacity and molecular binding.

引用

页码：214 / 224

页数：11

共 14 条

[1]

[Anonymous], KEGG PATHWAY DATABAS

[2]

FURNISS BS, 2005, VOGELS TXB PRACTICAL, P1102

[3] Synthesis and studies on some new fluorine containing triazolothiadiazines as possible antibacterial, antifungal and anticancer agents [J].

Holla, B. Shivarama ;

Rao, B. Sooryanarayana ;

Sarojini, B. K. ;

Akberali, P. M. ;

Kumari, N. Suchetha .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2006, 41 (05) :657-663

[4] The many roles of computation in drug discovery [J].

Jorgensen, WL .

SCIENCE, 2004, 303 (5665) :1813-1818

[5]

KEDAR NP, 2002, J AM COLL NUTR, V21, P506

[6] The radical scavenger edaravone enhances the anti-tumor effects of CPT-11 in murine colon cancer by increasing apoptosis via inhibition of NF-κB [J].

Kokura, S ;

Yoshida, N ;

Sakamoto, N ;

Ishikawa, T ;

Takagi, T ;

Higashihara, H ;

Nakabe, N ;

Handa, O ;

Naito, Y ;

Yoshikawa, T .

CANCER LETTERS, 2005, 229 (02) :223-233

[7]

MATH P, 2000, J BIOL CHEM, V275, P19439

[8] Synthesis of some new biologically active 1,3,4-oxadiazolyl nitroindoles and a modified Fischer indole synthesis of ethyl nitro indole-2-carboxylates [J].

Narayana, B ;

Ashalatha, BV ;

Raj, KKV ;

Fernandes, J ;

Sarojini, BK .

BIOORGANIC & MEDICINAL CHEMISTRY, 2005, 13 (15) :4638-4644

[9] High speed synthesis of pyrazolones using microwave-assisted neat reaction technology [J].

Pal, Sarbani ;

Mareddy, Jyoti ;

Devi, Nalla Suneetha .

JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY, 2008, 19 (06) :1207-1214

[10] Efficient inhibition of the Alzheimer's disease β-secretase by membrane targeting [J].

Rajendran, Lawrence ;

Schneider, Anja ;

Schlechtingen, Georg ;

Weidlich, Sebastian ;

Ries, Jonas ;

Braxmeier, Tobias ;

Schwille, Petra ;

Schulz, Joerg B. ;

Schroeder, Cornelia ;

Simons, Mikael ;

Jennings, Gary ;

Knoelker, Hans-Joachim ;

Simons, Kai .

SCIENCE, 2008, 320 (5875) :520-523

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