Alafeefy Ahmed M
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Arzneimittelforschung. 2008;58(9):457-63. doi: 10.1055/s-0031-1296539.
A series of fenamate quinazolinyl analogues, viz acids 6a-d, esters 6e-h, carbohydrazides 7a-d, arylidenes 8a-d, oxadiazol-2-ones 13a-d and oxadiazol-2-thiones 14a-d, have been prepared and screened for their analgesic (acetic acid-induced writhing), anti-inflammatory (carrageenan-induced rat paw edema) activities as well as their ulcerogenic effects. All the final compounds except 7a-d and 8a-d showed good dual activities. Compounds 6a, 6b, 6e, 6f, 13a and 14a showed activities comparable to that of mefenamic acid (CAS 61-68-7) in the acetic acid-induced writhing model as well as in the carrageenan-induced rat paw edema test at a dose level of 100 mg/ kg.Compounds 6a and 6b were highly ulcerogenic, while compounds 6e, 6f, 13a and 14a exhibited the lowest ulcerogenic effects.
已制备了一系列芬那酸喹唑啉基类似物,即酸6a - d、酯6e - h、碳酰肼7a - d、亚芳基8a - d、恶二唑 - 2 - 酮13a - d和恶二唑 - 2 - 硫酮14a - d,并对其镇痛(乙酸诱导扭体)、抗炎(角叉菜胶诱导大鼠足爪水肿)活性以及致溃疡作用进行了筛选。除7a - d和8a - d外,所有最终化合物均表现出良好的双重活性。在乙酸诱导扭体模型以及剂量为100 mg/kg的角叉菜胶诱导大鼠足爪水肿试验中,化合物6a、6b、6e、6f、13a和14a表现出与甲芬那酸(CAS 61 - 68 - 7)相当的活性。化合物6a和6b具有高度致溃疡作用,而化合物6e、6f、13a和14a表现出最低的致溃疡作用。