Savelli F, Boido A, Satta M, Peana A
Istituto di Scienze Farmaceutiche, Universita di Genova, Italy.
Farmaco. 1996 Feb;51(2):141-3.
Some new imidazolinyl-pyrazoles (4) were synthesized by condensation of 2-imidazolylhydrazine hydroiodid (1a) with beta-ketoesters to afford the intermediate 3 that, as free base, ring closes only to 4. The attempt to obtain the imidazo-triazepinone 5, starting from 2-imidazolinyl-2-methylhydrazine, was accomplished, in low yield, only in reacting with ethyl acetoacetate. The pharmacological evaluation of antiinflammatory and analgesic activities of pyrazoles 4a-f revealed an appreciable antiinflammatory activity.
通过2-咪唑基肼氢碘酸盐(1a)与β-酮酯缩合合成了一些新的咪唑啉基吡唑(4),得到中间体3,该中间体作为游离碱,仅环合生成4。从2-咪唑啉基-2-甲基肼开始制备咪唑并三氮杂庚三酮5的尝试,仅在与乙酰乙酸乙酯反应时以低产率完成。对吡唑4a-f的抗炎和镇痛活性进行药理评价,结果显示其具有明显的抗炎活性。