Synthesis and biological evaluation of novel pyrazole compounds

被引：42

作者：

Youssef, Amal M. ^{[2
,3
]}

Neeland, Edward G. ^{[2
]}

Villanueva, Erika B. ^{[1
]}

White, M. Sydney ^{[1
]}

El-Ashmawy, Ibrahim M. ^{[4
]}

Patrick, Brian ^{[5
]}

Klegeris, Andis ^{[1
]}

Abd-El-Aziz, Alaa S. ^{[2
]}

机构：

[1] Univ British Columbia Okanagan, Dept Biol, Kelowna, BC, Canada

[2] Univ British Columbia Okanagan, Dept Chem, Kelowna, BC, Canada

[3] Univ Alexandria, Fac Pharm, Dept Pharmaceut Chem, Alexandria, Egypt

[4] Univ Alexandria, Fac Vet Med, Dept Pharmacol, Alexandria, Egypt

[5] Univ British Columbia, Xray Facil, Vancouver, BC V5Z 1M9, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 15期

基金：

加拿大自然科学与工程研究理事会;

关键词：

Pyrazoles; Anti-inflammatory drugs; Neuroprotection; POTENTIAL PURINE ANTAGONISTS; DNA GYRASE INHIBITORS; P38-ALPHA MAP-KINASE; ANTIBACTERIAL ACTIVITY; CYTO-TOXICITY; DERIVATIVES; AGENTS; PYRAZOLO<3,4-D>PYRIMIDINES; IDENTIFICATION; PROLIFERATION;

D O I：

10.1016/j.bmc.2010.06.018

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：

A novel dipyrazole ethandiamide compound and acid chloride of pyrazolo[3,4-d] pyrimidine 4(5H)-one were prepared and reacted with a number of nucleophiles. The resultant novel compounds were tested in several in vitro and in vivo assays. Three compounds inhibited the secretion of neurotoxins by human THP-1 monocytic cells at concentrations that were not toxic to these cells. They also partially inhibited both cyclooxygenase-1 and -2 isoforms. In animal studies, two compounds were notable for their anti-inflammatory activity that was comparable to that of the clinically available cyclooxygenase-2 inhibitor celecoxib. Modeling studies by using the molecular operating environment module showed comparable docking scores for the two enantiomers docked in the active site of cyclooxygenase-2. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：5685 / 5696

页数：12

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