Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 37, Issue 8, Pages 689-697Publisher
EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/S0223-5234(02)01340-5
Keywords
N-substituted anthranilic acid-oxadiazolyl-pyrazolines; thiadiazolyl-pyrazolines; synthesis; albino rats; acute toxicity; anti-inflammatory activity; ulcerogenic activity
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The new 5-bromo-N-[2'-amino(1-acetyl-5substitutedaryl-2-pyrazolin-3-yl)-1',3',4'-oxadiazol-5'-ylmethyl]anthranilic acids 7a-7e and N-[2'-amino-(1-acetyl-5-substiutedaryl-2-pyrazolin-3-yl)-1',3',4'-thiadiazol-5'-ylmethyl]anthranilic acids 6'a-6'c have been synthesised from 5-bromo-N-(2'-aminosubstituedbenzylideneacetyl-1',3',4'-oxadiazol-5'-ylmethyl)anthranilic acids 6a-6e and N-(2'-aminosubstitutedbenzylideneacetyl-1',3',4'-thiadiazol-5'-ylmethyl)anthranilic acids 5'a-5'e, respectively. All these compounds have been screened in vivo for their anti-inflammatory and acute toxicity. Compounds 7b and 6'b were found to be potent member of this series, which showed 50.66 and 47.56%, respectively, inflammation inhibitory activity at a dose of 50 mg kg(-1) p.o., while standard drug, phenylbutazone, exhibited 45.52% anti-inflammatory activity at the same dose. However, 5-bromo-N-{2-amino[1-acetyl-5-(para-methoxyphenyl)-2-pyrazolin-3-yl]-1',3',4'-oxidiazol-5'-ylmethyl}anthranilic acid (7b) was found to be the most active and less ulcerogenic compound than the standard drag mid rest of the compounds of this series. The structures of these compounds have been established by IR, H-1-NMR spectroscopic data and elemental analyses. (C) 2002 Editions scientifiques et medicales Elsevier SAS. All rights reserved.
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