CAS: 3115-21-7; 4-Acetylpyridine Thiosemicarbazone

📜4-乙酰吡啶,氨基硫脲置于溶剂黄146体系中,用 乙醇 用作溶剂,化学反应生成(1-吡啶-4-基乙亚基氨基)硫脲
参考文献:氨基硫脲衍生物作为抗丝虫剂的设计,合成和体外评价
标题:氨基硫脲衍生物作为抗丝虫剂的设计,合成和体外评价
摘要:有效的杀大型丝蚴药物在市场上无法买到,为了寻找新的大型杀蛔虫剂,在这项研究工作中,制备了氨基硫脲衍生物并针对成年狗尾丝虫(一种牛丝虫寄生虫)进行了测试,作为丝虫寄生虫的模型线虫,班氏乌切菌.Lipinski 和 Veber 规则已被用于设计这些分子,并发现所有设计的分子都显示出类似药物的分子特性.氨基硫脲对s. Digitata的体外抗丝虫潜力使用蠕虫运动和 3-[4,5-二甲基噻唑-2-基]-2,5-二苯基溴化四唑 (Mtt) 还原比色测定法在 100 μg/ml 浓度下进行 24 小时的孵育期.目前用于丝虫的标准药物阿苯达唑,伊维菌素和乙胺嘧啶均不能有效杀灭成虫.相比之下,在第 3 位和第 4 位具有三氟甲基取代的苯基氨基硫脲,2-吡咯基和靛红基使成虫无法活动,并且还显示出 69%-83% 的甲臜形成抑制,这是无活力的指标.
Doi:10.1016/j.Exppara.2022.108363

专利信息

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-10814013-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

专利号:US-2008107598-A1
优先权日:2006-10-05
标 题:Efficient Synthesis of Chelators for Nuclear Imaging and Radiotherapy: Compositions and Applications

专利号:EP-2079486-A2
优先权日:2006-10-05
标题:Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

专利号:US-2013039853-A1
优先权日:2006-10-05
标题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

专利号:WO-2008045604-A2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications