Microwave-assisted Synthesis of 2-Styrylquinoline-4-carboxylic Acids as Antitubercular Agents
作者:Gisela C. Muscia、Silvia E. Asis、Graciela Y. Buldain
DOI:10.2174/1573406412666160901102710
日期:2017.7.11
BACKGROUND Many 2-substituted quinolines and especially 2-arylvinyl derivatives isolated from plants or prepared by synthesis have been designed from ethnopharmacological studies. OBJECTIVE In order to explore new aspects of the structure-antituberculosis activity relationship, a series of styrylquinoline derivatives was prepared. METHOD A series of styrylquinoline derivatives was prepared from quinaldic
背景技术从种族药理学研究中已经设计出许多从植物分离或通过合成制备的2-取代的喹啉,尤其是2-芳基乙烯基衍生物。目的为探索结构与抗结核活性关系的新方面,制备了一系列苯乙烯基喹啉衍生物。方法在环保条件下,通过Knoevenagel反应和三氟乙酸(TFA)作为催化剂,由喹啉酸和各种芳基苯甲醛制备了一系列苯乙烯基喹啉衍生物。结果该产品在较短的反应时间内获得了良好的收率,并通过美国国家过敏和传染病研究所(NIAID)评估了其对结核分枝杆菌H37Rv(Mtb)的生长抑制活性。