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HERO ID
1858881
Reference Type
Book/Book Chapter
Title
Synthesis, Biological Evaluation of Some 2,3-dihydropyrazoles and Thiazoles as Anti-inflammatory and Antibacterial Agents
Author(s)
Elgazwy, ASSH; Nassar, E; Zaki, MY
Year
2012
Publisher
OMICS Publishing Group
Volume
1
Issue
5 (2012)
Page Numbers
1.
Abstract
The present article describes the synthesis of two novel series of 5-(benzofuran-2-yl)-3-(4-(piperidin-1-yl)phenyl)- 2,3-dihydropyrazole-1-carbothioamide 6 and 1-(4-(3-(benzofuran-2-yl)-2-(4-arylthiazol-2-yl)-2,5-dihydro-1H-py r azol-5-yl)phenyl)piperidine 8a,b. All the newly synthesized target compounds (3, 4, 5, 6 8a and 8b) were screened for their in vivo anti-inflammatory (AI) activity using carrageenan-induced rat paw edema assay and in vitro antibacterial activity against two Gram-positive and two Gram-negative bacteria. All six compounds (3, 4, 5, 6, 8a, and 8b) showed consistently excellent AI activity ( greater than or equal to 70% inhibition), at 3 and 4 h after the carrageenan injection, comparable to that of standard drug indomethacin (78%) whereas the remaining twelve compounds have shown significant activity with 57-75% inhibition after 3 h and 56-63% inhibition after 4 h. All the tested compounds showed moderate antibacterial properties.
Keywords
Antibacterial activity; carrageenans; Gram-negative bacteria; Edema; thiazoles; Drugs; Inflammation; Indomethacin; Antibacterial agents
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