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New 2(1H)-quinoxalinones and their hexahydro derivatives were prepared for investigating their antimicrobial and antiinflammatory activities. The study showed that thiosemicarbazide 6a derived from the hexahydro-2(1H)-quinoxalinone series has nearly the same antibacterial activity as the reference drug ciprofloxacin. Moreover, the 2(1H)-quinoxalinones bearing N-phenyltriazole (9a) or 4-chlorophenyl-2,3-dihydrothiazole (13b) moieties were the most active ones after 4 h with use of the rat hind paw edema method, whereas their antiinflammatory and ulcerogenic activities were comparable with the selective COX-2 inhibitor celecoxib.

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Starting from isatoic anhydrides, several new 2,3-dihydroquinazolin-4(1H)-one derivatives bearing chalcone or pyrazole or thiazole moieties at the third position were synthesized. The analgesic and anti-inflammatory activities for most compounds were studied at a dose level of 50 mg/kg via the acetic-acid-induced writhing-response method and carrageenan-induced edema method, respectively. The study showed that the chalcones bearing a 4-chlorophenyl group 4c or 4-nitrophenyl group 4b were the most active ones as analgesics. Both chalcone 4c and N-phenyl pyrazole bearing 4-methoxy phenyl group 5b showed a higher anti-inflammatory activity than celecoxib but still lower than that of diclofenac sodium. Moreover, the chalcone 4c has nearly the same ulcerogenic index as the selective cyclooxygenase-2 inhibitor celecoxib.

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