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一种由通用有机催化剂四丁基氟化铵催化的4-吡喃喹啉酮衍生物的高效合成及其药理筛选。

An efficient synthesis of 4-pyrano quinolinone derivatives catalysed by a versatile organocatalyst tetra--butylammonium fluoride and their pharmacological screening.

作者信息

Prasad Pratibha, Shobhashana Pratik G, Patel Manish P

机构信息

Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, Gujarat 388120, India.

出版信息

R Soc Open Sci. 2017 Nov 29;4(11):170764. doi: 10.1098/rsos.170764. eCollection 2017 Nov.

Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1da/5717643/4eaddc233f55/rsos170764-g1.jpg

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