Saravanan G, Alagarsamy V, Prakash C R
Bapatla College of Pharmacy, Jawaharlal Nehru Technological University, Hyderabad, Andhra Pradesh, India.
Drug Discov Ther. 2012 Apr;6(2):78-87.
A new series of N'-((1-(substituted amino)methyl)-2-oxoindolin-3-ylidene)-4-(2-(methyl/phenyl)-4-oxoquinazolin-3(4H)-yl)benzohydrazide derivatives 4a-4l were designed and synthesized from anthranilic acid. All the synthesized compounds were characterized by spectroscopic means and elemental analyses. The tail-flick technique and the carrageenan-induced foot paw edema test were performed for screening analgesic and anti-inflammatory activity, respectively. All of the compounds were also examined for their ulcerogenicity. Some of the compounds showed significant activity. Among the test compounds, 4b exhibited 53% and 69% analgesic activity at a dose of 10 and 20 mg/kg, respectively. It also displayed 47% (10 mg/kg) and 65% (20 mg/kg) anti-inflammatory activity with one-fourth of ulcer index of the reference drugs diclofenac and aspirin.
从邻氨基苯甲酸设计并合成了一系列新的N'-((1-(取代氨基)甲基)-2-氧代吲哚啉-3-亚基)-4-(2-(甲基/苯基)-4-氧代喹唑啉-3(4H)-基)苯甲酰肼衍生物4a - 4l。所有合成的化合物均通过光谱手段和元素分析进行了表征。分别采用甩尾法和角叉菜胶诱导的足爪肿胀试验来筛选镇痛和抗炎活性。所有化合物还进行了致溃疡作用检测。部分化合物显示出显著活性。在受试化合物中，4b在剂量为10和20 mg/kg时分别表现出53%和69%的镇痛活性。它还显示出47%（10 mg/kg）和65%（20 mg/kg）的抗炎活性，且溃疡指数仅为参比药物双氯芬酸和阿司匹林的四分之一。
