Prasad Pratibha, Shobhashana Pratik G, Patel Manish P
Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, Gujarat 388120, India.
R Soc Open Sci. 2017 Nov 29;4(11):170764. doi: 10.1098/rsos.170764. eCollection 2017 Nov.
A new series of indole-based pyranoquinoline derivatives has been synthesized by a one-pot cyclocondensation reaction of 2-(4-substituted)phenyl--allyl-indole-3-carbaldehydes ; active methylenes ; and 4-hydroxy-1-substituted quinolin-2(1)-one catalysed by an organocatalyst tetra--butylammonium fluoride (TBAF) in aqueous ethanol. The easy experimental procedure of the reaction leads to excellent yields of pyranoquinoline derivatives. All the compounds were screened against a representative panel of bacteria and fungi. Some of the compounds are found to be equipotent or more potent than standard drugs as evident from the structural activity relationship study.
通过2-(4-取代苯基)-烯丙基吲哚-3-甲醛、活性亚甲基和4-羟基-1-取代喹啉-2(1)-酮在有机催化剂四丁基氟化铵(TBAF)催化下于乙醇水溶液中进行一锅环缩合反应,合成了一系列新的吲哚基吡喃并喹啉衍生物。该反应简便的实验步骤使得吡喃并喹啉衍生物的产率很高。所有化合物均针对一组代表性的细菌和真菌进行了筛选。从构效关系研究可以看出,一些化合物与标准药物具有同等效力或更高效力。