Bhalla M, Srivastava V K, Bhalla T N, Shanker K
Department of Pharmacology and Therapeutics, King George's Medical College, Lucknow, India.
Arzneimittelforschung. 1993 May;43(5):595-600.
6,8-Disubstituted-2-methyl-3-[2-substituted-indol-3-yl-methyl(ene)imino] -quinazoline-4(3H)-ones (III), 6,8-disbustituted-2-methyl-3-[2-substituted-indol-3-yl methyl amino]-quinazoline-4(3H)-ones (IV), 6,8-disubstituted-2-methyl-2-[5-(2-substituted-indol-3-yl)-thiazolidine- 3- one]quinazoline-4(3H)-ones (V), propionic acid derivative of 6,8-disubstituted-2-methyl-3-[5-(2-substituted indol-3-yl)-thiazolidine-3-one]-quinazoline-4(3H)-ones (VI), 6,8-disubstituted-2-methyl-3-[5-(2-substituted-indol-3-yl)-2-substituted benzylidine-thiazolidine-3-one]-quinazoline 4(3H)-ones (VII), 6,8-disubstituted-2-methyl-3-[2-substituted-indol-3-yl-4- chloroazetidine-1-one]-quinazoline-4-(3H)-ones (VIII), and 6,8-disubstituted-2-methyl-3-[2-substituted-indol-3- yl-alpha-arylazo methylimino]-quinazoline-4(3H)-ones (IX) were synthesized and evaluated for their anti-inflammatory activity against carrageenin induced paw oedema. The compounds found potent were further tested for their anti-writhmogenic activity in albino mice. The compounds exhibiting significant anti-inflammatory activity also showed marked protection against aconitine induced writhing response. The low toxicity of the potent compounds was also reflected by their high approximate LD50 values.
6,8 - 二取代 - 2 - 甲基 - 3 - [2 - 取代 - 吲哚 - 3 - 基甲基（亚甲基）亚氨基] - 喹唑啉 - 4(3H) - 酮（III）、6,8 - 二取代 - 2 - 甲基 - 3 - [2 - 取代 - 吲哚 - 3 - 基甲氨基] - 喹唑啉 - 4(3H) - 酮（IV）、6,8 - 二取代 - 2 - 甲基 - 2 - [5 - (2 - 取代 - 吲哚 - 3 - 基) - 噻唑烷 - 3 - 酮]喹唑啉 - 4(3H) - 酮（V）、6,8 - 二取代 - 2 - 甲基 - 3 - [5 - (2 - 取代 - 吲哚 - 3 - 基) - 噻唑烷 - 3 - 酮] - 喹唑啉 - 4(3H) - 酮的丙酸衍生物（VI）、6,8 - 二取代 - 2 - 甲基 - 3 - [5 - (2 - 取代 - 吲哚 - 3 - 基) - 2 - 取代苄叉基 - 噻唑烷 - 3 - 酮] - 喹唑啉4(3H) - 酮（VII）、6,8 - 二取代 - 2 - 甲基 - 3 - [2 - 取代 - 吲哚 - 3 - 基 - 4 - 氯氮杂环丁烷 - 1 - 酮] - 喹唑啉 - 4 - (3H) - 酮（VIII）以及6,8 - 二取代 - 2 - 甲基 - 3 - [2 - 取代 - 吲哚 - 3 - 基 - α - 芳基偶氮甲亚氨基] - 喹唑啉 - 4(3H) - 酮（IX）被合成，并针对角叉菜胶诱导的爪肿胀进行抗炎活性评估。发现有活性的化合物进一步在白化小鼠中测试其抗扭体活性。表现出显著抗炎活性的化合物对角叉菜碱诱导的扭体反应也显示出明显的保护作用。有效化合物的低毒性也通过其较高的近似半数致死量值体现出来。
