Microwave Assisted Facile Cleavage of 2,4-Dinitrophenylhydrazones to the Corresponding Carbonyl Compounds with N,N′-Dibromo-N,N′-1,2-ethanediylbis(p-toluenesulphonamide)
背景技术对现有抗微生物剂的致病性耐药性的惊人增加是一个严重的问题,并且这些细菌感染的治疗正变得越来越具有挑战性。因此,迫切需要开发新型抗微生物剂。目的作为我们正在进行的新型抗菌剂研究的一部分,一系列(Z)-5-((3-苯基-1H-吡唑-4-基)亚甲基)-2-的合成和抗菌活性在这项研究中将讨论噻吩并噻唑烷-4-酮衍生物。方法设计,合成(Z)-5-((3-苯基-1H-吡唑-4-基)亚甲基)-2-硫代噻唑烷酮-4-一衍生物,并评价其抗菌活性。通过IR,1 H NMR,13 C NMR和质谱确认结构。使用96孔微量滴定板和系列稀释方法在体外评估所有合成的化合物,以获得对多种不同菌株(包括耐多药临床分离株)的最低抑菌浓度(MIC)值。结果体外抗菌测试表明,系列7和9中的大多数化合物对厌氧菌(变形链球菌)菌株均表现出显着的抑制活性,MIC值为1 µg / mL。化合物7c和9c对MRSA的活性最高(3
Efficient and Highly Aldehyde Selective Wacker Oxidation
作者:Peili Teo、Zachary K. Wickens、Guangbin Dong、Robert H. Grubbs
DOI:10.1021/ol301240g
日期:2012.7.6
A method for efficient and aldehyde-selective Wackeroxidation of aryl-substituted olefins using PdCl2(MeCN)2, 1,4-benzoquinone, and t-BuOH in air is described. Up to a 96% yield of aldehyde can be obtained, and up to 99% selectivity can be achieved with styrene-related substrates.
Three series of 1,3-diaryl pyrazole derivatives bearing aminoguanidine or furan-2-carbohydrazide moieties have been synthesized, characterized and evaluated for antibacterial and anti-inflammatory activities. Most of the synthesized compounds showed potent inhibition of several Gram-positive bacterial strains (including multidrug-resistant clinical isolates) and Gram-negative bacterial strains with minimum inhibitory concentration values in the range of 1-64 mu g/mL. Compounds 6g, 6l and 7l presented the most potent inhibitory activity against Gram-positive bacteria (e.g. Staphylococcus aureus 4220), Gram-negative bacteria (e.g. Escherichia coli 1924) and the fungus, Candida albicans 7535, with minimum inhibitory concentration values of 1 or 2 mu g/mL. Compared with previous studies, these compounds exhibited a broad spectrum of inhibitory activity. Furthermore, compound 7l showed the greatest anti-inflammatory activity (93.59% inhibition, 30 min after intraperitoneal administration), which was more potent than the reference drugs ibuprofen and indomethacin. (C) 2015 Elsevier Ltd. All rights reserved.