Pande K, Tangri K K, Bhalla T N, Ahmad S, Dhasmana A, Barthwal J P
Pharmacology. 1984;29(4):193-7. doi: 10.1159/000138012.
Sixteen new 1,2-disubstituted-4-(indol-3'-yl)methylene imidazol-5-ones were synthesized by the condensation of oxazolone with different aryl amines and evaluated as to their anti-inflammatory and antiproteolytic activities. These derivatives showed 2-38% protection against carrageenin-induced paw oedema in albino rats at a dose of 100 mg/kg p.o. All compounds showed antiproteolytic activity. The degree of inhibition against trypsin-induced hydrolysis of casein ranged from 10 to 75% at a concentration of 4 X 10(-4) mol/l. Furthermore, active compounds of the series were also screened for their analgesic activity against aconitine-induced writhing in albino mice. The toxicity of the compounds was reflected by their approximate LD50 values.
通过恶唑酮与不同芳基胺的缩合反应合成了16种新型的1,2 - 二取代 - 4 -（吲哚 - 3'-基）亚甲基咪唑 - 5 - 酮，并对其抗炎和抗蛋白水解活性进行了评估。这些衍生物在100mg/kg口服剂量下，对白化大鼠角叉菜胶诱导的爪肿胀显示出2 - 38%的保护作用。所有化合物均显示出抗蛋白水解活性。在4×10（-4）mol/l的浓度下，对胰蛋白酶诱导的酪蛋白水解的抑制程度为10%至75%。此外，还筛选了该系列活性化合物对白化小鼠乌头碱诱导的扭体反应的镇痛活性。化合物的毒性通过其近似的LD50值反映出来。
