Syntheses of 2-aryl-4-(3-thienyl)imidazole derivatives with antiinflammatory properties.
作者:MAMORU SUZUKI、SADAO MAEDA、KAZUO MATSUMOTO、TOHRU ISHIZUKA、YOSHIO IWASAWA
DOI:10.1248/cpb.34.3111
日期:——
A series of 2-substituted 4-(3-thienyl)imidazoles (6, 11, and 14) was synthesized and evaluated for antiinflammatory activity. Among them, 6g, 14a, and 14g exhibited strong activity, comparable to that of ibuprofen. The acute toxicity and the ulcerogenicity were low as compared with those of standard acidic antiinflammatory agents. The structure-activity relationships are discussed.
研究人员合成了一系列 2-取代的 4-(3-噻吩基)咪唑(6、11 和 14),并对其抗炎活性进行了评估。其中,6g、14a 和 14g 具有很强的活性,与布洛芬的活性相当。与标准酸性消炎药相比,它们的急性毒性和致溃疡性较低。本文讨论了结构-活性关系。