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xABSTRACTThere have been renewed interests in the biological activities of carboxamides (benzamides), which are strong candidates for the development of new antimalarial, antifungal, anticonvulsant, anti-inflammatory and analgesic agents. Recent research has also shown that piperidine-4-carboxamides have potent anti-HIV-1 activity.The reaction of sodium borohydride with phthalimide derivatives in methanol: water (6:1), which is an improved synthetic method, afforded some novel 2-hydroxymethylbenzamides. Furthermore, the ring opening of phthalimide derivatives using amines (isopropylamine and benzylamine) in appropriate solvents (dimethylformamide or dichloromethane or methanol) resulted in the formation of new carboxamides. The percentage yields were generally high. All the novel compounds synthesized were unequivocally characterized by infra-red, nuclear magnetic resonance (1H and 13C), mass spectrophotometer and elemental analyses.The carboxamides were evaluated pharmacologically for their in-vivo anti-inflammatory and analgesic activities by carrageenan-induced rat paw oedema and acetic acid-induced writhing assay respectively. Some of the investigated compounds exhibited significant anti-inflammatory activity in the range of 42-76% in comparison to control, some of them also shown a promising analgesic activity in the range of 52-94% in comparison to control. 2-Hydroxymethyl-N-cyclopentylbenzamide 90 exhibited the highest anti-inflammatory activity (i.e.at 60 mg/kg it caused 72% inhibition) while 2-hydroxymethyl-N- [4-(2-methoxyphenyl) piperazin-1-yl]-propylbenzamide 93 shown the highest analgesic activity of 94% inhibition even higher than the reference drug, but 4-benzamido-1-(4-(2-methoxyphenyl)-piperizin-1-yl)-butyl-2-(2-methylethyl)-carboxamide 99 revealed a 74% anti-inflammatory activity at 40mg/kg and 84% analgesic activity at 40mg/kg among the carboxamdes obtained using the amines and the effects were dose-dependent.
