Abstract
A number of amidine derivatives ( 3a– i) were synthesized by condensation of cyanopyridine and cyanopyrazine with sulfonylhydrazides in the presence of sodium methoxide. 2-Acetylpyridine and 4-acetylpyridine were condensed with sulfonylhydrazides by microwave irradiation in solid phase to give corresponding hydrazones ( 5a– d). Indole-3-carboxaldehyde was condensed with sulfonylhydrazides by refluxing in acetic acid to give corresponding condensation product ( 5e and f). All the compounds, that is, 3a– i and 5a– f were purified by crystallization or by column chromatography. Structures of all the synthesized compounds are supported by correct IR, 1H NMR, mass spectral and analytical data. Anti-inflammatory activity evaluation was carried out using carrageenin-induced paw oedema assay and compounds 3e, f and 5e exhibited good anti-inflammatory activity, that is 52%, 37% and 38% at 50 mg/kg po, respectively. Analgesic activity evaluation was carried out using acetic acid writhing assay and compounds 3a, c, e and 5f showed good analgesic activity, that is, 50%, 50%, 50% and 60% at 50 mg/kg po, respectively.
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