Maggio B, Daidone G, Raffa D, Plescia S, Mantione L, Catena Cutuli V M, Mangano N G, Caruso A
Dipartimento di Chimica e Tecnologie Farmaceutiche, Università degli Studi di Palermo, via Archirafi, 32, I-90123 Palermo, Italy.
Eur J Med Chem. 2001 Sep;36(9):737-42. doi: 10.1016/s0223-5234(01)01259-4.
Several new ethyl 1-methyl-5-(substituted 3,4-dihydro-4-oxoquinazolin-3-yl)-1H-pyrazole-4-acetates 2, substituted at 2 and, alternatively at, 6, 7 or 8 positions of the quinazolinone nucleus, were synthesised. The compounds were screened for their analgesic and antiinflammatory activities, acute toxicity and ulcerogenic effect. Substitution in the benzene moiety of the quinazolinone ring did not show any advantage for the analgesic activity, whereas it improved in some cases the antiinflammatory activity. Some compounds showed appreciable antiinflammatory activity and, at the same time, very low ulcerogenic index.
合成了几种新的1-甲基-5-（取代的3,4-二氢-4-氧代喹唑啉-3-基）-1H-吡唑-4-乙酸乙酯2，其在喹唑啉酮核的2位以及6、7或8位进行了取代。对这些化合物进行了镇痛、抗炎活性、急性毒性和致溃疡作用的筛选。喹唑啉酮环苯部分的取代对镇痛活性没有任何优势，而在某些情况下改善了抗炎活性。一些化合物表现出明显的抗炎活性，同时致溃疡指数非常低。
