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Analgesic, anticonvulsant and anti-inflammatory activities of some synthesized benzodiazipine, triazolopyrimidine and bis-imide derivatives
Faculty
Science
Year:
2009
Type of Publication:
Article
Pages:
4787-4792
Authors:
Amr, Abd El-Galil E, Abdalla, Mohamed M, Said, Said A, Sabry, Nermien M
DOI:
10.1016/j.ejmech.2009.07.013
Journal:
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Volume:
44
Research Area:
Pharmacology \& Pharmacy
ISSN
ISI:000272928600001
Keywords :
4-Phenyl-but-3-en-2-one, Triazolopyrimidines derivatives, Pharmacological screening
Abstract:
A series of diazipine, pyrimidine, fused triazolopyrimidine and imide derivatives were newly synthesized using 4-phenyl-but-3-en-2-one 1 as a starting material and compounds 2 and 9 are intermediates. Initially the acute toxicity of the compounds was assayed via the determination of their LD(50). All the compounds were interestingly less toxic than the reference drug. The pharmacological screening showed that many of these obtained compounds have good analgesic, anticonvulsant and anti-inflammatory activities comparable to Valdecoxib (R), Carbamazepine (R) and Predensilone (R) reference drugs. Regarding the protection against Carrageenan (R) induced edema, five compounds were found more potent than Prednisolone (R). On the other hand, in searching for COX-2 inhibitor, the inhibition of plasma PGE2 for the compounds were determined and four compounds were found more potent than Prednisolone (R). The detailed synthesis, spectroscopic data, pharmacological screening and acute toxicity LD(50) for the synthesized compounds were reported. (C) 2009 Elsevier Masson SAS. All rights reserved.
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